Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
Group of alkaloids containing a benzylpyrrole group (derived from TRYPTOPHAN)
Compounds formed by condensation of secologanin with tryptamine resulting in a tetrahydro-beta-carboline which is processed further to a number of bioactive compounds. These are especially found in plants of the APOCYNACEAE; LOGANIACEAE; and RUBIACEAE families.
An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.
A group of pyrido-indole compounds. Included are any points of fusion of pyridine with the five-membered ring of indole and any derivatives of these compounds. These are similar to CARBAZOLES which are benzo-indoles.
A plant genus of the family Apocynaceae. It is the source of VINCA ALKALOIDS, used in leukemia chemotherapy.
An enzyme that catalyzes the conversion of L-tryptophan and water to indole, pyruvate, and ammonia. It is a pyridoxal-phosphate protein, requiring K+. It also catalyzes 2,3-elimination and beta-replacement reactions of some indole-substituted tryptophan analogs of L-cysteine, L-serine, and other 3-substituted amino acids. (From Enzyme Nomenclature, 1992) EC
An enzyme that catalyzes the conversion of L-serine and 1-(indol-3-yl)glycerol 3-phosphate to L-tryptophan and glyceraldehyde 3-phosphate. It is a pyridoxal phosphate protein that also catalyzes the conversion of serine and indole into tryptophan and water and of indoleglycerol phosphate into indole and glyceraldehyde phosphate. (From Enzyme Nomenclature, 1992) EC
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Indolesulfonic acid used as a dye in renal function testing for the detection of nitrates and chlorates, and in the testing of milk.
Substituted thioglucosides. They are found in rapeseed (Brassica campestris) products and related cruciferae. They are metabolized to a variety of toxic products which are most likely the cause of hepatocytic necrosis in animals and humans.
Alkaloid isolated from seeds of Peganum harmala L., Zygophyllaceae. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic Parkinson disease in the 1920's.
A plant genus of the APOCYNACEAE or dogbane family. Alkaloids from plants in this genus have been used as tranquilizers and antihypertensive agents. RESERPINE is derived from R. serpentina.
A plant genus of the family APOCYNACEAE. It contains ellipticine.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Decarboxylated monoamine derivatives of TRYPTOPHAN.
The Madder plant family of the order Rubiales, subclass Asteridae, class Magnoliopsida includes important medicinal plants that provide QUININE; IPECAC; and COFFEE. They have opposite leaves and interpetiolar stipules.
A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.
A group of indole-indoline dimers which are ALKALOIDS obtained from the VINCA genus of plants. They inhibit polymerization of TUBULIN into MICROTUBULES thus blocking spindle formation and arresting cells in METAPHASE. They are some of the most useful ANTINEOPLASTIC AGENTS.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Acetic acid derivatives of the heterocyclic compound indole. (Merck Index, 11th ed)
Attachment of isoprenoids (TERPENES) to other compounds, especially PROTEINS and FLAVONOIDS.
Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed)
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
A plant family of the order Theales.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
Benzoic acids, salts, or esters that contain an amino group attached to carbon number 2 or 6 of the benzene ring structure.
An enzyme that, in the pathway of cholesterol biosynthesis, catalyzes the condensation of isopentenyl pyrophosphate and dimethylallylpyrophosphate to yield pyrophosphate and geranylpyrophosphate. The enzyme then catalyzes the condensation of the latter compound with another molecule of isopentenyl pyrophosphate to yield pyrophosphate and farnesylpyrophosphate. EC
An enzyme that catalyzes the chlorination of a range of organic molecules, forming stable carbon-chloride bonds. EC
An indole-dione that is obtained by oxidation of indigo blue. It is a MONOAMINE OXIDASE INHIBITOR and high levels have been found in urine of PARKINSONISM patients.
A plant genus of the family APOCYNACEAE. Members contain echitovenidine, echitamine, venenatine (an indole alkaloid), and anti-inflammatory triterpenoids
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.
Compounds with a core of 10 carbons generally formed via the mevalonate pathway from the combination of 3,3-dimethylallyl pyrophosphate and isopentenyl pyrophosphate. They are cyclized and oxidized in a variety of ways. Due to the low molecular weight many of them exist in the form of essential oils (OILS, VOLATILE).
Inorganic or organic compounds derived from phosphine (PH3) by the replacement of H atoms. (From Grant & Hackh's Chemical Dictionary, 5th ed)
Ring compounds having atoms other than carbon in their nuclei. (Grant & Hackh's Chemical Dictionary, 5th ed)
Any chemical species which accepts an electron-pair from a LEWIS BASE in a chemical bonding reaction.
A biogenic amine that is found in animals and plants. In mammals, melatonin is produced by the PINEAL GLAND. Its secretion increases in darkness and decreases during exposure to light. Melatonin is implicated in the regulation of SLEEP, mood, and REPRODUCTION. Melatonin is also an effective antioxidant.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A N-hydroxylated derivative of 2-ACETYLAMINOFLUORENE that has demonstrated carcinogenic action.
Toxins isolated from any species of the seaweed Lyngbya or similar chemicals from other sources, including mollusks and micro-organisms. These have been found to be potent tumor promoters. They are biosynthesized from TRYPTOPHAN; VALINE; and METHIONINE nonribosomally (PEPTIDE BIOSYNTHESIS, NUCLEIC ACID-INDEPENDENT).
Covalent attachment of HALOGENS to other compounds.
The immediate precursor in the biosynthesis of SEROTONIN from tryptophan. It is used as an antiepileptic and antidepressant.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
Rhodium. A hard and rare metal of the platinum group, atomic number 45, atomic weight 102.905, symbol Rh. (Dorland, 28th ed)
A substance occurring in the urine of mammals and also in blood plasma as the normal metabolite of tryptophan. An increased urinary excretion of indican is seen in Hartnup disease from the bacterial degradation of unabsorbed tryptophan.
A plant genus of the family APOCYNACEAE that contains bisindole alkaloids and IBOGAINE.
Substances used for the detection, identification, analysis, etc. of chemical, biological, or pathologic processes or conditions. Indicators are substances that change in physical appearance, e.g., color, at or approaching the endpoint of a chemical titration, e.g., on the passage between acidity and alkalinity. Reagents are substances used for the detection or determination of another substance by chemical or microscopical means, especially analysis. Types of reagents are precipitants, solvents, oxidizers, reducers, fluxes, and colorimetric reagents. (From Grant & Hackh's Chemical Dictionary, 5th ed, p301, p499)
Compounds used extensively as acetylation, oxidation and dehydrating agents and in the modification of proteins and enzymes.
Chemical agents that increase the rate of genetic mutation by interfering with the function of nucleic acids. A clastogen is a specific mutagen that causes breaks in chromosomes.
A subclass of iridoid compounds that include a glucoside moiety, usually found at the C-1 position.
Techniques used in studying bacteria.
Determination of the spectra of ultraviolet absorption by specific molecules in gases or liquids, for example Cl2, SO2, NO2, CS2, ozone, mercury vapor, and various unsaturated compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A plant genus of the family RUBIACEAE. Members contain uncarine and other cytotoxic and hypotensive oxindole alkaloids.
One of several indole alkaloids extracted from Tabernanthe iboga, Baill. It has a complex pharmacological profile, and interacts with multiple systems of neurotransmission. Ibogaine has psychoactive properties and appears to modulate tolerance to opiates.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
Measurement of the intensity and quality of fluorescence.
A family of gram-negative, facultatively anaerobic, rod-shaped bacteria that do not form endospores. Its organisms are distributed worldwide with some being saprophytes and others being plant and animal parasites. Many species are of considerable economic importance due to their pathogenic effects on agriculture and livestock.
The reaction of two molecular entities via oxidation usually catalyzed by a transition metal compound and involving dioxygen as the oxidant.
The dogbane family of the order Gentianales. Members of the family have milky, often poisonous juice, smooth-margined leaves, and flowers in clusters. Asclepiadacea (formerly the milkweed family) has been included since 1999 and before 1810.
Compounds in which a methyl group is attached to the cyano moiety.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
A class of compounds composed of repeating 5-carbon units of HEMITERPENES.
Alkaloids extracted from various species of Cinchona.
Any liquid or solid preparation made specifically for the growth, storage, or transport of microorganisms or other types of cells. The variety of media that exist allow for the culturing of specific microorganisms and cell types, such as differential media, selective media, test media, and defined media. Solid media consist of liquid media that have been solidified with an agent such as AGAR or GELATIN.
Any salt or ester of glycerophosphoric acid.
A family of isomeric, colorless aromatic hydrocarbon liquids, that contain the general formula C6H4(CH3)2. They are produced by the destructive distillation of coal or by the catalytic reforming of petroleum naphthenic fractions. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Polymers where the main polymer chain comprises recurring amide groups. These compounds are generally formed from combinations of diamines, diacids, and amino acids and yield fibers, sheeting, or extruded forms used in textiles, gels, filters, sutures, contact lenses, and other biomaterials.
A genus of GRAM-POSITIVE ENDOSPORE-FORMING RODS in the family Paenibacillaceae.
A plant genus of the family Cruciferae. It contains many species and cultivars used as food including cabbage, cauliflower, broccoli, Brussel sprouts, kale, collard greens, MUSTARD PLANT; (B. alba, B. junica, and B. nigra), turnips (BRASSICA NAPUS) and rapeseed (BRASSICA RAPA).
A plant genus of the family RUBIACEAE. Members contain psychotridine and brachycerine (indole alkaloids).
Hydrocarbons with at least one triple bond in the linear portion, of the general formula Cn-H2n-2.
Widely distributed enzymes that carry out oxidation-reduction reactions in which one atom of the oxygen molecule is incorporated into the organic substrate; the other oxygen atom is reduced and combined with hydrogen ions to form water. They are also known as monooxygenases or hydroxylases. These reactions require two substrates as reductants for each of the two oxygen atoms. There are different classes of monooxygenases depending on the type of hydrogen-providing cosubstrate (COENZYMES) required in the mixed-function oxidation.
The five-carbon building blocks of TERPENES that derive from MEVALONIC ACID or deoxyxylulose phosphate.
A type of MONOTERPENES, derived from geraniol. They have the general form of cyclopentanopyran, but in some cases, one of the rings is broken as in the case of secoiridoid. They are different from the similarly named iridals (TRITERPENES).
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
Concentrated pharmaceutical preparations of plants obtained by removing active constituents with a suitable solvent, which is evaporated away, and adjusting the residue to a prescribed standard.
Cyclic esters of acylated BUTYRIC ACID containing four carbons in the ring.
A plant genus of the family BRASSICACEAE that is an ingredient of the preparation PC-SPES that is used to treat PROSTATIC HYPERPLASIA.
Placing of a hydroxyl group on a compound in a position where one did not exist before. (Stedman, 26th ed)
Organic compounds containing carbon and hydrogen in the form of an unsaturated, usually hexagonal ring structure. The compounds can be single ring, or double, triple, or multiple fused rings.
A genus of gram-negative, facultatively anaerobic, rod-shaped bacteria whose organisms occur in the lower part of the intestine of warm-blooded animals. The species are either nonpathogenic or opportunistic pathogens.
The rate dynamics in chemical or physical systems.
A group of alicyclic hydrocarbons with the general formula R-C5H9.
A technology, in which sets of reactions for solution or solid-phase synthesis, is used to create molecular libraries for analysis of compounds on a large scale.
The study of the structure, preparation, properties, and reactions of carbon compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
A genus of root and butt rot fungi in the family Tricholomataceae that produce rhizomorphs and are facultatively parasitic. Many species are pathogenic to trees causing Armillaria root disease.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
Any of the hormones produced naturally in plants and active in controlling growth and other functions. There are three primary classes: auxins, cytokinins, and gibberellins.
A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).
The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
The characteristic three-dimensional shape of a molecule.
A group of compounds derived from ammonia by substituting organic radicals for the hydrogens. (From Grant & Hackh's Chemical Dictionary, 5th ed)
Enzymes that hydrolyze O-glucosyl-compounds. (Enzyme Nomenclature, 1992) EC 3.2.1.-.
A phenomenon where microorganisms communicate and coordinate their behavior by the accumulation of signaling molecules. A reaction occurs when a substance accumulates to a sufficient concentration. This is most commonly seen in bacteria.
A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.
A genus of gram-negative, facultatively anaerobic, rod-shaped bacteria whose organisms arrange singly, in pairs, or short chains. This genus is commonly found in the intestinal tract and is an opportunistic pathogen that can give rise to bacteremia, pneumonia, urinary tract and several other types of human infection.
The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Anaerobic degradation of GLUCOSE or other organic nutrients to gain energy in the form of ATP. End products vary depending on organisms, substrates, and enzymatic pathways. Common fermentation products include ETHANOL and LACTIC ACID.
Tests of chemical substances and physical agents for mutagenic potential. They include microbial, insect, mammalian cell, and whole animal tests.
Methods used for the chemical synthesis of compounds. Included under this heading are laboratory methods used to synthesize a variety of chemicals and drugs.
The covalent bonding of an alkyl group to an organic compound. It can occur by a simple addition reaction or by substitution of another functional group.
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria that occurs in soil, fecal matter, and sewage. It is an opportunistic pathogen and causes cystitis and pyelonephritis.
Gram-negative gas-producing rods found in feces of humans and other animals, sewage, soil, water, and dairy products.
The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
A computer simulation technique that is used to model the interaction between two molecules. Typically the docking simulation measures the interactions of a small molecule or ligand with a part of a larger molecule such as a protein.
A dioxygenase with specificity for the oxidation of the indoleamine ring of TRYPTOPHAN. It is an extrahepatic enzyme that plays a role in metabolism as the first and rate limiting enzyme in the kynurenine pathway of TRYPTOPHAN catabolism.
The usually underground portions of a plant that serve as support, store food, and through which water and mineral nutrients enter the plant. (From American Heritage Dictionary, 1982; Concise Dictionary of Biology, 1990)
A plant genus of the family ARACEAE. Members contain beta-glucosidases and trypsin inhibitors.
Eighteen-carbon cyclopentyl polyunsaturated fatty acids derived from ALPHA-LINOLENIC ACID via an oxidative pathway analogous to the EICOSANOIDS in animals. Biosynthesis is inhibited by SALICYLATES. A key member, jasmonic acid of PLANTS, plays a similar role to ARACHIDONIC ACID in animals.
A plant genus of the family LOGANIACEAE (classified by some botanists as Gelsemiaceae). The sometimes used common name of trumpet flower is also used for DATURA.
A serotype of Salmonella enterica that is a frequent agent of Salmonella gastroenteritis in humans. It also causes PARATYPHOID FEVER.

Induction of AT-specific DNA-interstrand crosslinks by bizelesin in genomic and simian virus 40 DNA. (1/9500)

Bizelesin is a bifunctional AT-specific DNA alkylating drug. Our study characterized the ability of bizelesin to induce interstrand crosslinks, a potential lethal lesion. In genomic DNA of BSC-1 cells, bizelesin formed from approx. 0.3 to 6.03+/-0.85 interstrand crosslinks per 106 base pairs, at 5-100 nM drug concentration, respectively, comparable to the number of total adducts previously determined in the same system (J.M. Woynarowski, M.M. McHugh, L.S. Gawron, T.A. Beerman, Biochemistry 34 (1995) 13042-13050). Bizelesin did not induce DNA-protein crosslinks or strand breaks. A model defined target, intracellular simian virus 40 (SV40) DNA, was employed to map at the nucleotide level sites of bizelesin adducts, including potential interstrand crosslinks. Preferential adduct formation was observed at AT tracts which are abundant in the SV40 matrix associated region and the origin of replication. Many sites, including each occurrence of 5'-T(A/T)4A-3', co-mapped on both DNA strands suggesting interstrand crosslinks, although monoadducts were also formed. Bizelesin adducts in naked SV40 DNA were found at similar sites. The localization of bizelesin-induced crosslinks in AT-rich tracts of replication-related regions is consistent with the potent anti-replicative properties of bizelesin. Given the apparent lack of other types of lesions in genomic DNA, interstrand crosslinks localized in AT-rich tracts, and to some extent perhaps also monoadducts, are likely to be lethal effects of bizelesin.  (+info)

Prior exposure to neurotrophins blocks inhibition of axonal regeneration by MAG and myelin via a cAMP-dependent mechanism. (2/9500)

MAG is a potent inhibitor of axonal regeneration. Here, inhibition by MAG, and myelin in general, is blocked if neurons are exposed to neurotrophins before encountering the inhibitor; priming cerebellar neurons with BDNF or GDNF, but not NGF, or priming DRG neurons with any of these neurotrophins blocks inhibition by MAG/myelin. Dibutyryl cAMP also overcomes inhibition by MAG/myelin, and cAMP is elevated by neurotrophins. A PKA inhibitor present during priming abrogates the block of inhibition. Finally, if neurons are exposed to MAG/myelin and neurotrophins simultaneously, but with the Gi protein inhibitor, inhibition is blocked. We suggest that priming neurons with particular neurotrophins elevates cAMP and activates PKA, which blocks subsequent inhibition of regeneration and that priming is required because MAG/myelin activates a Gi protein, which blocks increases in cAMP. This is important for encouraging axons to regrow in vivo.  (+info)

Single synaptic events evoke NMDA receptor-mediated release of calcium from internal stores in hippocampal dendritic spines. (3/9500)

We have used confocal microscopy to monitor synaptically evoked Ca2+ transients in the dendritic spines of hippocampal pyramidal cells. Individual spines respond to single afferent stimuli (<0.1 Hz) with Ca2+ transients or failures, reflecting the probability of transmitter release at the activated synapse. Both AMPA and NMDA glutamate receptor antagonists block the synaptically evoked Ca2+ transients; the block by AMPA antagonists is relieved by low Mg2+. The Ca2+ transients are mainly due to the release of calcium from internal stores, since they are abolished by antagonists of calcium-induced calcium release (CICR); CICR antagonists, however, do not depress spine Ca2+ transients generated by backpropagating action potentials. These results have implications for synaptic plasticity, since they show that synaptic stimulation can activate NMDA receptors, evoking substantial Ca2+ release from the internal stores in spines without inducing long-term potentiation (LTP) or depression (LTD).  (+info)

Role of dexamethasone dosage in combination with 5-HT3 antagonists for prophylaxis of acute chemotherapy-induced nausea and vomiting. (4/9500)

Dexamethasone (20 mg) or its equivalent in combination with 5-HT3 antagonists appears to be the gold-standard dose for antiemetic prophylaxis. Additional to concerns about the use of corticosteroids with respect to enhanced tumour growth or impaired killing of the tumour cells, there is evidence that high-dosage dexamethasone impairs the control of delayed nausea and emesis, whereas lower doses appear more beneficial. To come closer to the most adequate dose, we started a prospective, single-blind, randomized trial investigating additional dosage of 8 or 20 mg dexamethasone to tropisetron (Navoban), a 5-HT3 receptor antagonist, in cis-platinum-containing chemotherapy. After an interim analysis of 121 courses of chemotherapy in 69 patients, we have been unable to detect major differences between both treatment alternatives. High-dose dexamethasone (20 mg) had no advantage over medium-dose dexamethasone with respect to objective and subjective parameters of acute and delayed nausea and vomiting. In relation to concerns about the use of corticosteroids in non-haematological cancer chemotherapy, we suggest that 8 mg or its equivalent should be used in combination with 5-HT3 antagonists until further research proves otherwise.  (+info)

Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. (5/9500)

LY315920 is a potent, selective inhibitor of recombinant human, group IIA, nonpancreatic secretory PLA2 (sPLA2). In a chromogenic isolated enzyme assay, LY315920 inhibited sPLA2 activity with an IC50 of 9 +/- 1 nM or 7.3 x 10(-6) mole fraction, which approached the stiochiometric limit of this assay. The true potency of LY315920 was defined using a deoxycholate/phosphatidylcholine assay with a mole fraction of 1.5 x 10(-6). LY315920 was 40-fold less active against human, group IB, pancreatic sPLA2 and was inactive against cytosolic PLA2 and the constitutive and inducible forms of cyclooxygenase. Human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells was inhibited by LY315920 with an IC50 of 0.79 microM. The release of TXA2 from these cells by N-formyl-methionyl-leucyl-phenylalanine or arachidonic acid was not inhibited. The i.v. administration of LY315920, 5 min before harvesting the bronchoalveolar lavage cells, resulted in the inhibition of sPLA2-induced production of TXA2 with an ED50 of 16.1 mg/kg. Challenge of guinea pig lung pleural strips with sPLA2 produced contractile responses that were suppressed in a concentration-dependent manner by LY315920 with an apparent KB of 83 +/- 14 nM. Contractile responses induced by arachidonic acid were not altered. Intravenous or oral administration of LY315920 to transgenic mice expressing the human sPLA2 protein inhibited serum sPLA2 activity in a dose-related manner over a 4-h time course. LY315920 is a potent and selective sPLA2 inhibitor and represents a new class of anti-inflammatory agent designated SPI. This agent is currently undergoing clinical evaluation and should help to define the role of sPLA2 in various inflammatory disease states.  (+info)

Glomerular size-selective dysfunction in NIDDM is not ameliorated by ACE inhibition or by calcium channel blockade. (6/9500)

BACKGROUND: In patients with insulin-dependent diabetes mellitus (IDDM) and overt nephropathy glomerular barrier size-selectivity progressively deteriorates with time and is effectively improved by angiotensin converting enzyme (ACE) inhibition. Whether similar glomerular functional changes develop in proteinuric patients with non-insulin-dependent diabetes mellitus (NIDDM), and whether antihypertensive agents can favorably affect glomerular filtration of macromolecules in these patients, has not been documented yet. METHODS: We investigated renal hemodynamics and fractional clearance of neutral dextrans of graded sizes, in nine proteinuric patients with NIDDM and renal biopsy findings of typical diabetic glomerulopathy. Six healthy volunteers served as controls. We also investigated the effects of an ACE inhibitor and of a calcium channel blocker, both given in doses targeted to achieve a comparable level of systemic blood pressure control, on glomerular hemodynamics and sieving function. Theoretical analysis of glomerular macromolecule transport was adopted to evaluate intrinsic glomerular membrane permeability properties. RESULTS: Fractional clearance of large macromolecules (42 to 66 A in radius) was significantly higher in diabetic patients than in controls, and the distribution of membrane pore radii was calculated to be shifted towards larger pore sizes in diabetics (mean radius increased from 55 to 60 A). Despite effective blood pressure control, neither antihypertensive affected glomerular hemodynamics to any significant extent. Fractional clearance of dextrans, as well as of albumin and IgG, and total urinary proteins were not modified by either treatments. CONCLUSIONS: These data indicate that patients with NIDDM and overt nephropathy develop abnormalities in size-selective function of the glomerular barrier and, at variance to IDDM, such changes were not ameliorated either by ACE inhibition or calcium channel blockade.  (+info)

Involvement of p21 in the PKC-induced regulation of the G2/M cell cycle transition. (7/9500)

Activation of protein kinase C (PKC) inhibits cell cycle progression at the G1/S and G2/M transitions. We found that phorbol 12-myristate 13-acetate (PMA) induced upregulation of p21, not only in MCF-7 cells arrested in the G1 phase as previously shown, but also in cells delayed in the G2 phase. This increase in p21 in cells accumulated in the G1 and G2/M phases of the cell cycle after PMA treatment was inhibited by the PKC inhibitor GF109203X. This indicates that PKC activity is required for PMA-induced p21 upregulation and cell cycle arrest in the G1 and G2/M phases of the cell cycle. To further assess the role of p21 in the PKC-induced G2/M cell cycle arrest independently of its G1 arrest, we used aphidicolin-synchronised MCF-7 cells. Our results show that, in parallel with the inhibition of cdc2 activity, PMA addition enhanced the associations between p21 and either cyclin B or cdc2. Furthermore, we found that after PMA treatment p21 was able to associate with the active Tyr-15 dephosphorylated form of cdc2, but this complex was devoid of kinase activity indicating that p21 may play a role in inhibition of cdc2 induced by PMA. Taken together, these observations provide evidence that p21 is involved in integrating the PKC signaling pathway to the cell cycle machinery at the G2/M cell cycle checkpoint.  (+info)

Phosphatidylinositol 3-kinase and protein kinase C are required for the inhibition of caspase activity by epidermal growth factor. (8/9500)

The mechanism by which growth factors exert an anti-apoptotic function on many cell types is not well understood. This issue is addressed in relation to epidermal growth factor (EGF) which inhibits apoptosis induced by staurosporine or wortmannin in an epithelial tumour cell line (CNE-2). The presence of EGF substantially reduced the in vitro Ac-DEVD-AMC hydrolytic activity and almost completely suppressed the intracellular cleavage of poly(ADP-ribose) polymerase in staurosporine- or wortmannin-treated cells. Staurosporine but not wortmannin caused the intracellular proteolytic processing of pro-caspase-3 and this event was transiently inhibited by EGF. Staurosporine-induced apoptosis was not inhibited by EGF in the presence of wortmannin or LY294002. Similarly, EGF failed to inhibit wortmannin-induced apoptosis in the presence of staurosporine, chelerythrine chloride or Go6850. These results suggest that phosphatidylinositol 3-kinase and protein kinase C play a role in the survival function of EGF but the reduction of cellular caspase activity cannot be satisfactorily explained by a lack of pro-caspase-3 activation.  (+info)

Molecular interactions between indole derivatives and 1,2-di-oleoyl-sn-glycero-3-phosphocholine (DOPC) were studied using a Nima Langmuir-Blodgett (LB) trough. A 0.25 M phosphate buffer sub-phase was used with a physiological pH range of 7.31-7.48. The air-phosphate buffer interface was examined at room temperature. Constant ionic strength was maintained by 0.100 M potassium chloride (KCl). Two different indole derivatives were used, indole and tryptophan, in concentrations of 3.0 uM and 5.0 uM. It is evident when examining the isotherms that the DOPC monolayer is expanded in the presence of indole derivatives, as the area per molecule was increased by 0.02nm2/molecule ...
the thesis entitled STUDIES ON DEVELOPING A FACILE ROUTE FOR THE SYNTHESIS OF HIGHLY SUBSTITUTED QUINOLINE AND INDOLE DERIVATIVES portrays our attempt to revisit the mechanism of 1,3- dipolar additions with a view to establishing whether it follows a concerted pathway or a stepwise reaction sequence through the formation of a zwitterionic intermediate, which will definitely contribute to the better use of this technique. Furthermore, we propose to develop novel routes for the synthesis of quinoline and indole derivatives with predefined substitution pattern. The thesis is devided into four ...
293392741 - EP 1100780 A1 2001-05-23 - 2,3,3a,4,9,9a-HEXAHYDRO-8-HYDROXY-1H-BENZ[F]INDOLES, A METHOD FOR THE PRODUCTION THEREOF, AND THEIR USE AS MEDICAMENTS - [origin: DE19834714A1] The application relates to substituted 2,3,3a,4,9,9a hexahydro-8-hydroxy-1H-benz[f]indole derivatives, to a method for the production thereof, and to their use as medicaments. The inventive indole derivatives correspond to general formula (1).[origin: DE19834714A1] The application relates to substituted 2,3,3a,4,9,9a hexahydro-8-hydroxy-1H-benz[f]indole derivatives, to a method for the production thereof, and to their use as medicaments. The inventive indole derivatives correspond to general formula (1).
It is prudent that novel classes of antibiotics be urgently developed to manage the WHO prioritized multi-drug resistant (MDR) pathogens posing an unprecedented medical crisis. Simultaneously, multiple essential proteins have to be targeted to prevent easy resistance development. An integration of structure-based virtual screening and ligand-based virtual screening was employed to explore the antimicrobial properties of indole derivatives from a compound database. Whole-genome sequences of the target pathogens were aligned exploiting DNA alignment potential of MAUVE to identify putative common lead target proteins. S-adenosyl methionine (SAM) biosynthesizing MetK was taken as the lead target and various literature searches revealed that SAM is a critical metabolite. Furthermore, SAM utilizing CobA involved in the B12 biosynthesis pathway, Dam in the regulation of replication and protein expression, and TrmD in methylation of tRNA were also taken as drug targets. The ligand library of 715 indole
1. An (aza)indole derivative represented by the general formula: ##STR00412## wherein T represents nitro, cyano or trifluoromethyl; ring J represents an aryl ring or a heteroaryl ring; Q represents carboxy, lower alkoxycarbonyl, carbamoyl, mono(di)(lower alkyl)carbamoyl, sulfo, sulfamoyl or 5-tetrazolyl; Y represents a hydrogen atom, amino, a halogen atom, nitro, optionally substituted lower alkyl or optionally substituted lower alkoxy with the proviso that two or more Y optionally exist on ring J and these Y are optionally the same or different from each other; X1, X2 and X3 independently represent CR2 or N with the proviso that all of X1, X2 and X3 do not represent N at the same time, and when two or more R2 exist, these R2 are optionally the same or different from each other; and R1 and R2 independently represent a halogen atom, cyano, perfluoro(lower alkyl), -AA, -A-D-E-G or --N(-D-E-G)2 with the proviso that two (-D-E-G) are optionally different from each other; in the formula, AA ...
Semantic Scholar extracted view of Catechol and indole derivatives in a transplantable islet-cell tumour of the golden hamster. by Lennart Cegrell et al.
1. A compound represented by Formula below, ##STR00021## wherein (1) R1 to R3 and X are the same or different, and each independently represents (1) a C.sub.6.about.C60 aryl group or a C.sub.5.about.C60 heterocyclic group substituted or unsubstituted with at least one selected from the group including hydrogen, a halogen group, a cyano group, a nitrile group, a C.sub.1.about.C60 alkyl group, a C.sub.1.about.C60 alkoxy group, a C.sub.1.about.C60 alkylamine group, a C.sub.1.about.C60 arylamine group, a C.sub.1.about.C60 alkylthiophene group, a C.sub.6.about.C60 arylthiophene group, a C.sub.2.about.C60 alkenyl group, a C.sub.2.about.C60 alkynyl group, a C.sub.3.about.C60 cycloalkyl group, a C.sub.6.about.C60 aryl group, a deuterium-substituted C.sub.6.about.C60 aryl group, a C.sub.8.about.C60 arylalkenyl group, a substituted or unsubstituted silane group, a substituted or unsubstituted boron group, a substituted or unsubstituted germanium group, and a substituted or unsubstituted C.sub.5.about.C60 ...
Principal Investigator:ISHIKURA Minoru, Project Period (FY):1997 - 1999, Research Category:Grant-in-Aid for Scientific Research (C), Section:一般, Research Field:Chemical pharmacy
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This patent search tool allows you not only to search the PCT database of about 2 million International Applications but also the worldwide patent collections. This search facility features: flexible search syntax; automatic word stemming and relevance ranking; as well as graphical results.
3,3′-Diindolylmethane (DIM), an indole derivative produced on consumption of broccoli and other cruciferous vegetables, has been shown to have multiple anticancer effects in both in vivo and in vitro models. The present study was carried out to clarify the mechanism of DIMs antiangiogenic activity. We found that DIM can inhibit vascular endothelial growth factor (VEGF)-induced cell proliferation and DNA synthesis in human umbilical vascular endothelial cells (HUVECs). Consistent with this inhibition, VEGF-induced extracellular signal-regulated kinase (ERK1/2) phosphorylation was greatly reduced. However, VEGF receptor phosphorylation induced by VEGF was not affected by DIM, indicating that DIM does not exert a direct and specific effect on the tyrosine kinase activity of this receptor. Further studies showed that DIM had a similar inhibitory effect on ERK1/2 phosphorylation induced by a variety of growth factors. Furthermore, Ras-GTP content, which dramatically increased after HUVECs were ...
A series of 3 beta-(p-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters (2) were synthesized and found to possess high affinity for the cocaine binding site in rat striatum. The p-chloro (2c) and p-iodo (2n) compounds, which were the most potent analogues prepared, were found to be 85 and 78 times more potent than (-)-cocaine. The p-bromo (2m) and p-methyl (2d) were also 56 and 60 times more potent than cocaine. QSAR and CoMFA studies were conducted to correlate binding affinity of the cocaine analogues with their structural features.
Given the importance of heterocycle indole derivatives, much effort has been directed toward the development of methods for functionalization of the indole nucleus at N1 and C3 sites. Moreover, the platinum-catalyzed allyation of nucleophiles was an established and efficient way, which has been applied to medicinal and organic chemistry. In our research, the platinum-catalyzed 2,3-disubstitued indoles with allylic acetates was investigated under different conditions. Herein, we established a simple, convenient, and efficient method, which afforded high yield of allylated indoles.
Proteins and nucleic acids absorb light in the near-UV due to the presence of aromatic heterocyclic chromophores. In this work linear dichroism (LD) in combination with fluorescence polarization anisotropy (FPA) and magnetic circular dichroism (MCD) is used to investigate electronic excitations and excited states of indole derivatives, purine derivatives, the wye base, 2-phenylindole and 4,6-diamidino-2-phenylindole (DAPI). The UV spectrum of indole, which is the chromophoric core of tryptophan, is resolved into contributions from the lowest nearly degenerate 1A1 --| 1La and 1A1 --| 1Lb transitions, and the moment directions for the four lowest transitions in indole and eight selected methyl and methoxy derivatives are determined. Substitution does not generally perturb the transition moment directions, with exception for the 1A1 --| 1Lb and 1A1 --| 1Bb transitions whose moment directions are significantly altered by a methoxy group in 4- or 6-position. The transition moment directions and the
Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus bearing a substituent in position 1, said substituent incorporating an acid, ester or amide function therein, are disclosed. The nucleus is further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7, 8, and 9. The derivatives are useful antiinflammatory, analgesic, antibacterial and antifungal agents and methods for their preparation and use are also disclosed.
Prenyl transfer reactions occur ubiquitously in nature and play an important role in primary and secondary metabolism in all domains of life. Prenylated secondary metabolites including indole alkaloids usually demonstrate improved biological and pharmacological activities and thus makes them to promising candidates for drug discovery and development. Important producers of such bioactive compounds are fungi of ascomycetes and bacteria of actinomycetes. The transfer reactions of a prenyl moiety from prenyl diphosphate, primarily dimethylallyl diphosphate (DMAPP), onto indole derivatives including tryptophan are mainly catalyzed in nature by the members of the dimethylallyltryptophan synthase (DMATS) superfamily. In the last years, remarkable progress has been achieved in their biochemical, molecular biological, and structural characterization, especially for DMATS enzymes from fungi. The major challenge of this thesis is to provide a better understanding of the catalytic features of these enzymes ...
About indomethacinnsaid, indole derivative, anti-inflammatory, potent antipyretic and analgesic.mechanism of action of indomethacinindomethacin acts b
About indomethacinnsaid, indole derivative, anti-inflammatory, potent antipyretic and analgesic.mechanism of action of indomethacinindomethacin acts b
Molecular interactions between indole derivatives and 1,2-di-oleoyl-sn-glycero-3-phosphocholine (DOPC) were studied using a Nima Langmuir-Blodgett (LB) trough. A 0.25 M phosphate buffer sub-phase was used with a physiological ...
VELASCO-BEJARANO, Benjamín et al. Diindolylmethane Derivatives as Apoptosis Inductors in L5178y Cells. J. Mex. Chem. Soc [online]. 2008, vol.52, n.3, pp.224-228. ISSN 1870-249X.. Cell growth and division are highly regulated processes, although a notable exception is provided by the cancer cell, which arises as a variant that has lost the usual proliferation control pathways. Consequently, there is growing interest in the search for antitu-moral substances with high efficacy, low toxicity, and minimum side effects. In this sense, we synthesize eight diindolylmethane derivatives and the in vitro antitumor activity against murine L5178Y lymphoma cells was assessed. The preliminary results showed that the substituent and its position on the phenyl group were important for its potency against the lymphoma cells tested. Compound 3a was the most active compound with 93 % cell grown inhibition and 71.04% of apoptosis.. Palabras clave : DIM derivatives; apoptosis; cytotoxic effects; L5178Y cells. ...
3-Methyl-7-azaindole 5654-93-3 NMR spectrum, 3-Methyl-7-azaindole H-NMR spectral analysis, 3-Methyl-7-azaindole C-NMR spectral analysis ect.
TY - JOUR. T1 - A survey of core replacements in indole-based HIV-1 attachment inhibitors. AU - Wang, Tao. AU - Wallace, Owen B.. AU - Zhang, Zhongxing. AU - Fang, Haiquan. AU - Yang, Zhong. AU - Robinson, Brett A.. AU - Spicer, Timothy P.. AU - Gong, Yi Fei. AU - Blair, Wade S.. AU - Shi, Pei-Yong. AU - Lin, Pin Fang. AU - Deshpande, Milind. AU - Meanwell, Nicholas A.. AU - Kadow, John F.. PY - 2019/1/1. Y1 - 2019/1/1. N2 - Indole- and azaindole-based glyoxylyl amide derivatives have been described as HIV-1 attachment inhibitors (AIs) that act by blocking the interaction between the viral gp120 coat protein and the human host cell CD4 receptor. As part of an effort to more deeply understand the role of the indole/azaindole heterocycle in the expression of antiviral activity, a survey of potential replacements was conducted using parallel synthesis methodology. The design and optimization was guided by a simple 2-dimensional overlay based on an overall planar topography between the ...
Disclosed is a novel, flame retarded, non-blooming nylon composition with excellent thermal stability. This composition is comprised of from about 5 to about 35 percent (by weight) of a condensation product derived from brominated phenol by the displacement of bromine from said phenol wherein: (a) said phenol is selected from the group consisting of tribromophenol, tetrabromophenol, pentabromophenol, and mixtures thereof; (b) said condensation product has a repeating structural unit of the formula ##STR1## WHEREIN A IS AN INTEGER OF FROM ABOUT 0 TO ABOUT 4, B IS AN INTEGER OF FROM ABOUT 0 TO ABOUT 2, C IS AN INTEGER OF FROM ABOUT 1 TO ABOUT 5, A PLUS B PLUS C EQUAL 5, Q is a monovalent bond from a carbon atom in the aromatic nucleus of said repeating structural unit to an oxygen atom bonded to an aromatic nucleus, and the polymeric units containing said repeating structural unit comprise at least 80 percent (by weight) of said product; (c) said condensation product contains from about 17 to about 31
Diindolylmethane Benefits as an Estrogen Blocking Supplement & Testosterone Booster. Effects on Weight Loss, Bodybuilding, PMS, Menopause, Cancer & More.
Diindolylmethane is suggested to balance levels of estrogen, creating a healthy hormone balance for both men and women. Effects can relieve...
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Trandolapril is the ethyl ester prodrug of a nonsulfhydryl angiotensin converting enzymeinhibitor, trandolaprilat. Trandolapril is chemically described as (2S, 3aR, 7aS)-1-[(S)-N-[(S)-1-Carboxy-3-phenylpropyl]alanyl] hexahydro-2-indo-linecarboxylic acid, 1-ethyl ester. Its empirical formula is C24H34N2O5and M.W.= 430.54
The α-aminoamide family of sodium ion channel blockers have exhibited analgesic effects on neuropathic pain. Here, a series of novel α-aminoamides containing an indole ring were designed and synthesized. These compounds were evaluated in mice using a formalin test and they exhibited significant anti-allodynia activities. However, the analgesic mechanism of these compounds remains unclear; a subset of the synthesized compounds can only moderately inhibit the sodium ion channel, Nav1.7, in a whole-cell patch clamp assay. Overall, these results suggest that introduction of an indole moiety to α-aminoamide derivatives can significantly improve their bioactivity and further study is warranted.
Genestra DIM- 60 capsules • Diindolylmethane (DIM) formulation • Provides 75 mg of 3,3-diindolylmethane per day • Convenient vegetable capsule format • Vegan formula • Dairy-free, gluten-free Each capsule of DIM provides 25 mg of 3,3-diindolylmethane. The recommended daily dosage is 3 capsules.
INDOLIN-6-AMINE | C8H10N2 | CID 34185 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Buy 4-Azaindole (CAS 272-49-1), a specialty product for proteomics research, from Santa Cruz. Molecular Formula: C7H6N2, Molecular Weight: 118.14
3-[(2-Fluorophenyl)(2-methyl-1H-indol-3-yl)methyl]-2-methyl-1H-indole | C25H21FN2 | CID 3612166 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Alfa Aesar™ 5-Nitro-3-(1,2,3,6-tetrahydro-4-pyridyl)indole, 97% 1g Alfa Aesar™ 5-Nitro-3-(1,2,3,6-tetrahydro-4-pyridyl)indole, 97% Heterocyclic...
5-Methyl-4-nitro-2,1,3-benzoselenadiazole (1) was converted into 1,2,5-selenadiazolo[3,4-g]indole (3) by the Batcho-Leimgruber indole synthesis. Subsequent deselenation afforded 6,7-diaminoindole (4) which on treatment with biacetyl afforded 2,3-dimethylpyrrolo[2,3-f]quinoxaline (5) in 80% yield from 3.. ...
Alfa Aesar™ 5-Bromo-3-(3-oxycyclopentyl)indole, 95% 1g Alfa Aesar™ 5-Bromo-3-(3-oxycyclopentyl)indole, 95% Bromomethylphenyl to Bromophenyla...
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2,3-dihydro-1H-indol-5-amine,dihydrochloride 2759-14-0 MSDS report, 2,3-dihydro-1H-indol-5-amine,dihydrochloride MSDS safety technical specifications search, 2,3-dihydro-1H-indol-5-amine,dihydrochloride safety information specifications ect.
Diindoylmethane is a molecule which is named after its structure, two indole groups attached to a methane group. It is commonly found in broccoli, and holds promise as being a molecule for anti-cancer effects and as an aromatase inhibitor.
55142-77-3 - PJYCVBMPEOJLKW-UHFFFAOYSA-N - Indole-3-carboxamide, N-(2-(hydroxy(3-indolyl)methylthio)ethyl)- - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Trandolapril information about active ingredients, pharmaceutical forms and doses by Ratiopharm, Trandolapril indications, usages and related health products lists
Buy DIM Diindolymethane Capsules. DIM Diindolymethane aids healthy estrogen metabolism and helps balance hormones for men and women. We offer it for only...
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Indole Derivatives Isolated from Brown Alga Sargassum thunbergii Inhibit Adipogenesis through AMPK Activation in 3T3-L1 Preadipocytes. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
Saracoglu Scheme 50 silica gel, which acts as a mild acidic catalyst, under microwave irradiation or room temperature gave unsymmetrical bis(indolyl)nitroethanes (236a-h) in excellent yields (69-86%) (Scheme 51 and Table 6). But, the conjugate addition of the indole derivatives 233-235 with 227 failed. This situation was attributed to the fact that silica gel is not sufficiently acidic to catalyze the desired Michael addition. In order to overcome this difficulty, the reactions of 2, 14, 19 and 228-235 with 220 were performed in acetonitrile under reflux using p-TsOH (25% wt) as the catalyst. Saracoglu Scheme 50 silica gel, which acts as a mild acidic catalyst, under microwave irradiation or room temperature gave unsymmetrical bis(indolyl)nitroethanes (236a-h) in excellent yields (69-86%) (Scheme 51 and Table 6). But, the conjugate addition of the indole derivatives 233-235 with 227 failed. This situation was attributed to the fact that silica gel is not sufficiently acidic to catalyze the ...
A number of N-hydroxylated indole derivatives have been fed to rats and the urinary metabolites compared with those obtained on feeding the corresponding N-H indoles. 1-Methoxy- and 1-acetoxy-indole were metabolized to compounds normally observed on feeding indole. 1-Hydroxy- and 1-methoxy-indole-3-carboxylic acids were both partially excreted unchanged and reduced to indole-3-carboxylic acid which was excreted along with its glucuronide. Indole-3-glyoxylic acid and its 1-methoxy derivative were excreted almost entirely unchanged. 1-Hydroxyindole-3-glyoxylic acid was mostly excreted unchanged, but some reduction to indole-3-glyoxylic acid took place. The stability of these acids is associated with their low pKa values. The significance of the removal in vivo of groups attached through oxygen to the 1 position of indoles in relation to the synthesis of new potential medicinal agents is noted.
Chemical investigations of two specimens of Trikentrion flabelliforme collected from Australian waters have resulted in the identification of four new indole alkaloids, trikentramides A-D (9-12). The planar chemical structures for 9-12 were established following analysis of 1D/2D NMR and MS data. The relative configurations for 9-12 were determined following comparison of 1H NMR data with previously reported and related natural products. The application of a quantum mechanical modeling method, density functional theory, confirmed the relative configurations and also validated the downfield carbon chemical shift observed for one of the quaternary carbons (C-5a) in the cyclopenta[g]indole series. The indole-2,3-dione motif present in trikentramides A-C is rare in nature, and this is the first report of these oxidized indole derivatives from a marine sponge ...
Infection with hepatitis B virus (HBV) is a major cause of liver diseases such as cirrhosis and hepatocellular carcinoma. In our previous studies, we identified indole derivatives that have anti-HBV activities. In this study, we optimize a series of 5-hydroxy-1H-indole-3-carboxylates, which exhibited potent anti-HBV
article{8518837, abstract = {The reaction of triazolinediones (TADs) and indoles is of particular interest for polymer chemistry applications, as it is a very fast and irreversible additive-free process at room temperature, but can be turned into a dynamic covalent bond forming process at elevated temperatures, giving a reliable bond exchange or transclick reaction. In this paper, we report an in-depth study aimed at controlling the TAD-indole reversible click reactions through rational design of modified indole reaction partners. This has resulted in the identification of a novel class of easily accessible indole derivatives that give dynamic TAD-adduct formation at significantly lower temperatures. We further demonstrate that these new substrates can be used to design a directed cascade of click reactions of a functionalized TAD moiety from an initial indole reaction partner to a second indole, and finally to an irreversible reaction partner. This controlled sequence of click and transclick ...
Indoleamine 2,3-dioxygenase (IDO) is an heme-containing enzyme involved in the regulation of important immunological responses and neurological processes. The enzyme catalyzes the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan (Trp) to yield N-formylkynurenine, that is the initial and rate limiting step of the kynurenine pathway. Some indole derivatives have been reported to act as effectors of the enzyme by enhancing its catalytic activity. On the basis of the recent availability of the crystal structure of IDO, in this work we investigate substrate recognition and enhancer binding to IDO using molecular docking experiments. In addition, conformational transitions of IDO in response to substrate and enhancer binding are studied using coarse graining simulations with the program FIRST. The results enable us to identify (i) the binding site of enhancer modulators; (ii) the motion of an electrostatic gate that regulates the access of the substrate to the catalytic site ...
TY - JOUR. T1 - Four Fatalities Involving 5-IT. AU - Seetohul, L. Nitin. AU - Pounder, Derrick J.. PY - 2013/9. Y1 - 2013/9. N2 - The new designer drug 5-(2-aminopropyl)indole (5-IT) is an indole derivative with stimulant properties. Its synthesis was first described by Albert Hofmann and Franz Troxler in 1962. We report four deaths associated with 5-IT and a validated high-performance liquid chromatography method for quantitation of the drug. In all four deaths, an autopsy was performed, and femoral venous blood, heart blood, urine and vitreous humor were submitted for toxicological analysis. The blood specimens were subjected to comprehensive testing that included alcohol analysis by headspace gas chromatography (GC-FID), acidic/neutral, basic drug and opiates screening by liquid chromatography-mass spectrometry (LC-MS-MS), and acidic/neutral, basic and acidic drugs screening by HPLC. In Case 1, a 25-year-old male, 3,4-methylenedioxymethamphetamine (MDMA; 10 mg/L) were detected, and death was ...
Although polar transport and the TIR1-dependent signaling pathway of the plant hormone auxin/indole-3-acetic acid (IAA) are well characterized, understanding of the biosynthetic pathway(s) leading to the production of IAA is still limited. Genetic dissection of IAA biosynthetic pathways has been complicated by the metabolic redundancy caused by the apparent existence of several parallel biosynthetic routes leading to IAA production. Valuable complementary tools for genetic as well as biochemical analysis of auxin biosynthesis would be molecular inhibitors capable of acting in vivo on specific or general components of the pathway(s), which unfortunately have been lacking. Several indole derivatives have been previously identified to inhibit tryptophan-dependent IAA biosynthesis in an in vitro system from maize endosperm. We examined the effect of one of them, 6-fluoroindole, on seedling development of Arabidopsis thaliana and tested its ability to inhibit IAA biosynthesis in feeding experiments ...
From the parotid secretion of the South African toad, Bufo regularis, the following principles have been isolated and studied pharmacologically:. A. Cholesterol.. B. Regularo-bufagin, C23H34O5, which has a digitalis-like action. The minimal emetic dose in pigeons is 0.3 mgm., that in cats 0.09 mgm., and the average fatal dose in cats is 0.15 mgm. per kilogram.. C. Regularo-bufotoxin, C37H60O10N4, which also has a digitalis-like action. The minimal emetic dose in pigeons is 0.35 mgm., that in cats 0.275 mgm., and the average fatal dose in 10 cats is 0.48 mgm. per kilogram. Both regularo-bufagin and -bufotoxin have a pressor action, and stimulate isolated smooth muscle organs. The cardiac action of regularo-bufotoxin seems to be relatively more persistent than that of regularo-bufagin.. D. Regularo-bufotenine, which is an indole derivative, in the form of a flavianate. It stimulates both the isolated rabbits intestines and guinea pigs uteri, and raises the arterial blood pressure, its activity ...
On the bound form of ascorbic acid. XVII. Biogenesis of ascorbigen, 3-indolylacetonitrile and other indole derivatives in Brassica oleracea L. from DL-tryptophan-3-14 ...
RATIONALE: Drugs used in chemotherapy, such as temozolomide, work in different ways to stop the growth of tumor cells, either by killing the cells or by stopping them from dividing. Sunitinib malate may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth and by blocking blood flow to the tumor. Giving temozolomide together with sunitinib malate may kill more tumor cells.. Phase II was never conducted due to toxicity in phase I.. PURPOSE: This phase I/II trial is studying the side effects and best dose of sunitinib malate when given together with temozolomide and to see how well they work in treating patients with stage III or stage IV malignant melanoma.. ...
This study is a Phase I trial in two parts. In part 1, an MTD to the combination of perifosine and sunitinib malate will be determined. In some previous trials with perifosine and other biologic agents, doses determined in Phase I studies are not as well tolerated in larger groups of patients when response is an endpoint. Thus in part 2, with the MTD as a starting point, a group of patients will be accrued with the goal of ensuring that they will be able to tolerate at least two courses of therapy, which would make them evaluable for response in a Phase II study. As a secondary endpoint, the effects of the combination of perifosine and sunitinib malate will be evaluated for response rate and time to progression. The pharmacokinetics of the combination of the study drugs will be measured.. For the purposes of this study, one cycle of therapy will be defined as 6 weeks. Patients will take one 50 mg tablet of perifosine one to three times a day and sunitinib malate once a day for 4 out of 6 weeks. ...
The Max Foundation is partnering with Pfizer on a pilot program for international product access for Sutent® (sunitinib malate) to help ensure that international prescription assistance requests are addressed consistently and objectively. The collaboration is designed to help patients outside of the U.S. living in lower-income economies, specifically uninsured and underinsured persons living where product is either not available commercially or significant access hurdles exist and where local market initiatives cannot address the request.. Requests for Sutent® (sunitinib malate) must meet specified criteria. View our global map and click on individual countries to learn where this collaboration is operating today. Contact us for more information about access to Sutent (sunitinib malate) in these countries. ...
Trandolapril is an ACE inhibitor used to treat high blood pressure, it may also be used to treat other conditions. It is marketed by Abbott Laboratories under the brand name Mavik. Trandolapril is a prodrug that is de-esterified to trandolaprilat. It is believed to exert its antihypertensive effect through the renin-angiotensin-aldosterone system. Trandolapril has a half-life of about 6 hours, and trandolaprilat has a half life of about 10 h. Trandolaprilat has about eight times the activity of its parent drug. About one-third of trandolapril and its metabolites are excreted in the urine, and about two-thirds of trandolapril and its metabolites are excreted in the feces. Serum protein binding of trandolapril is about 80%. Trandolapril acts by competitive inhibition of angiotensin converting enzyme (ACE), a key enzyme in the renin-angiotensin system which plays an important role in regulating blood pressure. Side effects reported for trandolapril include nausea, vomiting, diarrhea, headache, dry ...
3,3-Diindolylmethane (DIM) is a naturally occurring indole, which is currently under investigation as a potential chemopreventive agent. The concentrations of DIM in plasma, liver, kidney, lung, heart, and brain tissues were determined following oral administration of two different formulations to mice (250 mg/kg). Mice were sacrificed periodically from 0 to 24 h after administration of either a crystalline or an absorption-enhanced formulation (Bio-Response-DIM; Indolplex) of DIM, and plasma and tissue concentrations were determined by high-performance liquid chromatography (UV detection, 280 nm). A physiologically based pharmacokinetic (PBPK) model was developed to characterize the pharmacokinetic properties of the two different formulations. The final model included parameters reflecting linear first-order absorption, systemic clearance, and distributional clearance in the remainder compartment, which were considered independent of formulation. All pharmacokinetic profiles from the two ...
Despite the numerous constraints on p53 function in RCC [24-27], sunitinib treatment does induce the expression of several p53-dependent genes (e.g. NOXA, HDM2, p21waf) in RCC xenografts. The induction of these genes is, however, limited to the interval during which tumor growth is suppressed and is attenuated once resistance develops. Although several factors have been shown to block p53 transcriptional activity in RCC, these are for the most part stable genetic alterations (e.g. KR-POK expression) that are not known to be subject to regulation by hypoxia or other metabolic changes that occur during treatment with angiogenesis inhibitors.. The factor(s) responsible for the transient activation and subsequent inactivation of p53 transcriptional activity during the course of treatment with sunitinib are unknown but at least one well-characterized p53 transcriptional suppressant (i.e. HDMX) appears to be temporally linked to p53 function in our xenograft models and may therefore be a candidate. ...
3,3′-Diindolylmethane or DIM are phytochemicals derived from the digestion of indole-3-carbinol, belonging to the group of Indoles, found abundantly in broccoli, Brussels sprouts, cabbage and kale, etc. Health Benefits 1. Antiinflammatory and chemopreventive effects on Skin In the examination of the effects of 3,3′-Diindolylmethane (DIM) on antiinflammatory and antitumor promotion activity in mouse skin and …. ...
DIM (3,3-diindolylmethane), a small molecule compound, is a proposed cancer preventive agent that can be safely administered to humans in repeated doses. We report that administration of DIM in a multidose schedule protected rodents against lethal doses of total body irradiation up to 13 Gy, whethe …
Diindolylmethane (DIM) is a compound derived from the digestion of indole-3-carbinol, found in cruciferous vegetables such as broccoli, Brussels sprouts, cabbage and kale.
Two naturally occurring compounds from vegetables and soy slowed the spread of cancer cells in a new test-tube study. Researchers exposed breast and ovarian cancer cells to diindolylmethane (DIM), a compound that results from digesting vegetables such as broccoli and genistein, a soy isoflavone, and found that the compounds reduced the spread of cancer from cell to cell (metastasis) by 80% compared to cells that were not exposed. The doctors reported similar results using DIM and genistein on melanoma and prostate cancer cells, and noted that the amounts of the compounds are probably similar to high-dose supplements. DIM is also available as a supplement. Reference: ...
Indoles represent a structural element in a myriad of natural products and biologically active molecules. Of special importance are 2,3-disubstituted indoles. Thus, a number of methods for their synthesis have been described. However, these are often hampered by a number of limitations: they often offer poor regioselectivity and suboptimal functional group tolerance. Also, they can normally be adapted to the procurement of a small subclass of indoles only. We have developed an approach to 2,3-disubstituted indoles overcoming these obstacles. By selectively activating the amide carbonyl in isatin-derived oxindoles, we obtained a number of the title compounds in a regiospecific and functional group-tolerant manner. The methodology is normally characterized by excellent yields. The reaction proceeds by chemoselective partial reduction of the amide moiety to an iminium salt and a subsequent nucleophilic addition followed by dehydration, which furnishes the target indole. A number of nucleophiles, including
Renal cell carcinoma (RCC), the 13th most common malignancy worldwide, kills about 116,000 people annually (1). While early-stage RCC is treatable by surgical and other interventions, the metastatic form of this malignancy is chemotherapy-resistant and lethal (2). RCC comprises several distinct histologic varieties, of which clear cell (cc)RCC represents the dominant subtype and accounts for up to 85% of all RCC cases (3). Over the past decade, small-molecule therapies that target growth factor-, angiogenesis-, and nutrient-sensing pathways (e.g., the tyrosine kinase inhibitors sunitinib and sorafenib) have become the frontline treatment options for advanced RCCs (2, 4). Although most patients will derive some benefit from these agents, virtually all will experience significant side effects, eventually develop resistance, and ultimately succumb to metastatic disease within 5 years (5, 6). Treatment of advanced RCCs is therefore still a significant therapeutic challenge.. Before the introduction ...
Lipolysis (breakdown of stored fat) and thermogenesis (increased caloric expenditure) to reduce unwanted fat stores and increase lean muscle mass*. Diindolylmethane or DIM® is a plant compound that promotes estrogen metabolism causing a beneficial shift in the balance of estrogen, testosterone and progesterone in both men and women.* A healthy balance between estrogen, testosterone and progesterone supports skin, prostate, ovarian, breast, skeletal, joint and cardiovascular health, lean body mass, efficient fat burning, better physical conditioning, improved mood and memory, increased libido, and by reducing the effects of aging such as those found in menopause and prostate dysfunction.*. Banaba leaf extract contains corosolic acid, which supports cortisol balance, glucose transport into cells, normal blood sugar and insulin levels in the blood and reduces appetite.* The reduction in appetite, due to tighter control of blood sugar levels, may help support healthy weight management.* Banabas ...
Trials are being conducted to determine the authenticity of consuming Indole-3-Carbinol supplements to prevent illnesses, particularly cancer. Although it does not provide an active cure to cancer, Indole-3-Carbinol is scientifically proven to support the health of reproductive organs and cellular reproduction for both men and women. It also assists in detoxifying the intestines and liver.As an antioxidant, it stimulates the production of enzymes that detoxify toxins and protects cell structures including DNA. Lycopene is another vegetable antioxidant with proven health benefits.With possible anti-carcinogenic, antioxidant and anti-atherogenic effects, this vegetable component is only just being acknowledged as a solution to a variety of health issues Indole-3-Carbinol is currently being clinically researched as a cancer preventive agent by the National Institutes of Health.. Other names for Indole-3-Carbinol:. I3C, 3-Indolylcarbinol, 1H-Indole-3-methanol, 3-Hydroxymethyl Indole, 3 Hydroxymethyl ...
Effects of imatinib, flumatinib, and sunitinib on the phosphorylation of KIT, ERK1/2, and signal transducer and activator of transcription-3 (STAT3) in 32D-V559
Natures Way DIM-plus Diindolylmethane 120 Vegetarian Capsules DIM-plus Difference-Patented Complex- DIM-plus contains BioResponse-DIM Complex and its patented, enhanced bioavailability delivery system for diindolylmethane. Enhanced Absorption-The bioavailability of DIM-plus is superior to regular diidolylmethane and its unstable precursor, indole-3-carbinol (I3C). With DIM-plus you are assured a stabilized and consistent dose of diindolylmethane. Protectamins Vegetables-DIM-plus also contains spinach, cabbage and concentrated broccoli for additional phytonutrients. Recommendation: Women take 2 capsules daily with food. Men take 2 capsules twice daily with food. Men take 2 capusles twice daily with food. For intensive Use (Women/Men): take up to double the recommended dose. Caution: Do not if pregnant or lactating. A harmless but noticeable change in urine color may occur during usage. Supplement Facts Serving Size 2 Capules/Servings Per Container 60 Amount Per Serving %DV Vitamin E
ECHAs dossier evaluation process covers compliance checks and the examination of testing proposals. By consulting the table below, you can find out whether ECHA has started to evaluate dossiers for a particular substance and follow the progress through the evaluation process. The table below displays the type, scope and status of the assessment undertaken for a given dossier. The decision date and the non-confidential version of the decision are published shortly after the decision has been adopted. Before publishing the non-confidential version of an adopted decision on its website, ECHA consults the addressees of the decision on this version. ECHA systematically removes any personal data from the non-confidential version of a decision. Some sections may also be redacted based on justified claims by registrants, regarding information confidential or deemed to harm their commercial interest if disclosed. Check the expandable boxes below for more details. ...
Indol er en aromatisk heterosyklisk organisk forbindelse. Det har en bisyklisk struktur og består av en benzenring med seks medlemmer som er sammensmeltet med en nitrogenholdig pyrrolring med fem medlemmer. Deltakelsen av et enslig elektronpar av nitrogen i den aromatiske ringen medfører at indol ikke er en base, og det oppfører seg ikke som et usammensatt amin. Indol er et faststoff ved romtemperatur. Det forekommer naturlig i menneskelig avføring og har en intens fekal odør. I svært lave konsentrasjoner har det imidlertid en blomsterduft, og det er et innholdsstoff i mange blomsters duft (slik som appelsinblomst) og parfymer. Det forekommer også i steinkulltjære. Indolstrukturen kan gjenfinnes i mange organiske forbindelser slik som aminosyren tryptofan og i tryptofaninneholdende protein, i alkaloider og i pigmenter. Indol gjennomgår elektrofil substitusjon, hovedsakelig ved posisjon 3. Substituerte indoler er strukturelle elementer i (og for visse forbindelser det syntetiske ...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Indole 3 Carbinol Powder Manufacturers, Factory, Suppliers From China, We welcome customers, business associations and friends from all parts of the world to contact us and seek cooperation for mutual benefits.
5-Bromo-6-chloro-3-indolyl β-D-glucuronide cyclohexylammonium salt (Magenta-GlcA ); >= 98%; 5-Bromo-6-chloro-3-indolyl β-D-glucuronide cyclohexylammonium salt serves as a chromogenic substrate for β-glucuronidase and produces a magenta color in GUS (+) bacterial colonies;
This study determined the maximum tolerated dose and safety of SU011248 (sunitinib malate, SUTENT) in combination with FOLFOX [Leucovorin + Fluorouracil
DIM has the biological properties listed in the chart below. Because of its various potent anti-cancer properties, the National Cancer Institute of the United States has begun clinical trials of DIM as a therapeutic for numerous forms of cancer.[citation needed] Due to its innate immune modulating properties (potentiation of Interferon-Gamma receptors and production),[citation needed] DIM is also under investigation as a treatment for a variety of viral infections and antibiotic resistant bacteria.[citation needed] As DIM has been demonstrated to synergize with Interferon-Gamma in the potentiation of the MHC-I Complex,[citation needed] it is currently also under investigation as an adjuvant to IFN-G treatment models for both cancer and viral infections such as HIV, HPV and Hepatitis. ...
IAA, indole 3 acetic acid, IAA | indole 3 acetic acid, BSA conjugated, BSA conjugated IAA, BSA conjugated indole 3 acetic acid, IAA-BSA, AS16 3218
Description Dietary Supplement DIM is an indole phytochemical that is a natural metabolite of compounds found in cruciferous vegetables such as broccoli, Brussels sprouts and cabbage. In preclinical studies, DIM has been shown to lead to the preferential formation of estrogen metabolites that are correlated with health
In recent years, use of psychoactive synthetic stimulants has grown rapidly. 5-(2-Aminopropyl)indole (5-IT) is a synthetic drug associated with a number of fatalities, that appears to be one of the newest 3,4-methylenedioxymethamphetamine (MDMA) replacements. Here, the monoamine-releasing properties of 5-IT, its structural isomer 6-(2-aminopropyl)indole (6-IT), and MDMA were compared using in vitro release assays at transporters for dopamine (DAT), norepinephrine (NET), and serotonin (SERT) in rat brain synaptosomes.
Indole - Insanity Volume 14.6: Inscriptions - Ireland, William Henry Volume 14.7: Ireland - Isabey, Jean Baptiste ...
Indole: 6-API. Naphthalenes: Methamnetamine. *Naphthylaminopropane. Tetralin: 6-APT. Cyclized phenyl-. alkylamines. * ...
Indoles: 5-IT. *6-API. Naphthalenes: Methamnetamine. *Naphthylaminopropane. Tetralin: 6-APT. Cyclized phenyl-. alkylamines. * ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
... (also known as CBL-2201) is an indole-based synthetic cannabinoid that presumably has similar properties to the closely ... Report on a new designer drug: Napht-1-yl 1-(5-fluoropentyl)-1H-indole-3-carboxylate". Forensic Science International. 257: 209 ... New representatives of indol-3-carboxylates series and indazole-3-carboxylates as novel group of cannabinoids. Identification ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
b) 3-(1-naphthoyl)indole or 3-(1-naphthyl)indole with substitution at the nitrogen atom of the indole ring, whether or not ... g) N- adamantyl-indole-3-carboxamide, with substitution at the nitrogen atom of the indole ring, whether or not further ... f) indole- (2,2,3,3-tetramethylcyclopropyl)methanone, with substitution at the nitrogen atom of the indole ring, whether or not ... e) 3-phenylacetylindole or 3-benzoylindole with substitution at the nitrogen atom of the indole ring, whether or not further ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
N-[(1S)-1-(Aminocarbonyl)-2-methylpropyl]-1-[(4-fluorophenyl)methyl]-1H-indole-3-carboxamide ... September 2015). "Pharmacology of Indole and Indazole Synthetic Cannabinoid Designer Drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA ... "Four types of cannabimimetic indazole and indole derivatives, ADB-BINACA, AB-FUBICA, ADB-FUBICA, and AB-BICA, identified as ...
1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-3-[2-(4-morpholinyl)ethyl]-1H-indole ...
Indole-3-carboxylates. *5F-PB-22. *FDU-PB-22. *FUB-PB-22 ...
"Two new synthetic cannabinoids, AM-2201 benzimidazole analog (FUBIMINA) and (4-methylpiperazin-1-yl)(1-pentyl-1H-indol-3-yl) ...
5-chloro-3-ethyl-1H-indole-2-carboxylic acid [2-(4-piperidin-1-yl-phenyl)ethyl]amide ...
... and molecular modeling of novel 4-alkyloxy indole derivatives related to cannabimimetic aminoalkyl indoles (AAIs)". Bioorganic ... Huffman JW, Padgett LW (2005). "Recent developments in the medicinal chemistry of cannabimimetic indoles, pyrroles and indenes ... March 1991). "Antinociceptive (aminoalkyl)indoles". Journal of Medicinal Chemistry. 34 (3): 1099-110. doi:10.1021/jm00107a034. ...
Indole acetic acid derivative.. Reversible COX-1/COX-2 inhibitor.. PO and topical.. Bioavailability = 50-60%; protein binding ...
Ehrlich's reagent (indoles, etc). *Froehde reagent (opioids). *Gallic acid reagent (drug precursor) ...
1991). "Antinociceptive (aminoalkyl)indoles". J. Med. Chem. 34 (3): 1099-110. doi:10.1021/jm00107a034. PMID 1900533. Everett RM ... AM-630 (6-iodopravadoline) WIN 54,461 (6-bromopravadoline) WIN 55,212-2 RCS-4 (1-pentyl-3-(4-methoxybenzoyl)indole) Haubrich DR ... 1992). "Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists ...
... is an indole alkaloid and substituted tryptamine present in the plant Lespedeza bicolor. The alkaloid bears a close ... January 2001). "The chemistry of indoles. CIII. Simple syntheses of serotonin, N-methylserotonin, bufotenine, 5-methoxy-N- ... methyltryptamine, bufobutanoic acid, N-(indol-3-yl)methyl-5-methoxy-N-methyltryptamine, and lespedamine based on 1- ...
Indole: 6-API. Naphthalenes: Methamnetamine. *Naphthylaminopropane. Tetralin: 6-APT. Cyclized phenyl-. alkylamines. * ...
Indole: 6-API. Naphthalenes: Methamnetamine. *Naphthylaminopropane. Tetralin: 6-APT. Cyclized phenyl-. alkylamines. * ...
... indole negative, rod-shaped bacterium.[2] The bacterium is approximately 1-3 microns in length, and is capable of motility via ...
Indole: 6-API. Naphthalenes: Methamnetamine. *Naphthylaminopropane. Tetralin: 6-APT. Cyclized phenyl-. alkylamines. * ...
Mitragyna speciosa (kratom) indole derivatives: *Mitragynine. *Mitragynine pseudoindoxyl. Antagonists[edit]. *Buprenorphine. * ...
Gribble GW (9 October 2010). Heterocyclic Scaffolds II:: Reactions and Applications of Indoles. Springer Science & Business ...
Using C. elegans as a biosensor, we identified indole and several metabolites [e.g., indole-3-carboxaldehyde (ICA), indole ... K12ΔtnaA or K12ΔtnaA plus indole (Indole) vs. K12ΔtnaA plus vehicle (Vehicle). (C) Lifespan curves of N2 on K12ΔtnaA ... Indoles Extend Healthspan in C. elegans and Drosophila via AHR.. To identify genes mediating the effects of indoles on ... Indoles Derived from Commensal E. coli Extend Healthspan of C. elegans.. To investigate effects of indoles secreted by ...
Indole (fr); индолы (ru); Indol (sr-el); indole (en); インドール (ja); Indol (hu); Indol (ca); Індол (uk); 吲哚 (zh-tw); Indol (vi); ... Indol (id); Indol (nn); ഇൻഡോൾ (ml); Indol (sh); 인돌 (ko); Ինդոլ (hy); ಇಂಡೋಲ್ (kn); indol (pt); Indol (gl); إندول (ar); 吲哚 (zh- ... Indol (sv); אינדול (he); Indol (tk); 吲哚 (zh-hant); 吲哚 (zh-cn); Indoli (fi); Indolo (eo); Indol (cs); Indol (bs); indolo (it); ... Indol (nl); Индол (ru); C8H7N (it); C8H7N, اندول, الإندول, Indole (ar); 2,3-bentsopyrroli, Bentsopyrroli (fi); Indol, Indole ( ...
Navnet indol er avledet fra en kombinasjon av ordene indigo og oleum fordi indol til å begynne med ble isolert gjennom ... Sykloaddisjoner av indol[rediger , rediger kilde]. Bare C-2- og C-3-pi-bindingene i indol er i stand til ... Kjemiske reaksjoner med indol[rediger , rediger kilde]. Nitrogenbasiskhet[rediger , rediger kilde]. Selv om indol N-1 ... Oksidasjon av indol[rediger , rediger kilde]. Fordi indol er så rikt på elektroner, blir det lett oksidert. Enkle oksidanter ...
Bartoli indole synthesis Bischler-Möhlau indole synthesis Cadogan-Sundberg indole synthesis Fukuyama indole synthesis Gassman ... Indoles are susceptible to hydrogenation of the imine subunit. Indole-3-butyric acid Indole test Isoindole Isoindoline Martinet ... The Leimgruber-Batcho indole synthesis is an efficient method of synthesizing indole and substituted indoles. Originally ... Although the synthesis of indole itself is problematic using the Fischer indole synthesis, it is often used to generate indoles ...
Disclaimer: The information provided on HealthWorld Online is for educational purposes only and IS NOT intended as a substitute for professional medical advice, diagnosis, or treatment. Always seek professional medical advice from your physician or other qualified healthcare provider with any questions you may have regarding a medical condition ...
... is a indoles (CHEBI:24828) indole-3-acetonitrile (CHEBI:17566) is a nitrile (CHEBI:18379) ... indole-3-acetonitrile (CHEBI:17566) has role auxin (CHEBI:22676) indole-3-acetonitrile (CHEBI:17566) has role human xenobiotic ... indole-3-acetonitrile (CHEBI:17566) has role plant hormone (CHEBI:37848) indole-3-acetonitrile (CHEBI:17566) has role plant ... CHEBI:17566 - indole-3-acetonitrile. Main. ChEBI Ontology. Automatic Xrefs. Reactions. Pathways. Models. ...
Other names: 1H-Indole; Ketole; 1-Azaindene; 1-Benzazole; 2,3-Benzopyrrole; Benzopyrrole; Indol; 1-H-indol ...
Some 200 dimeric indole alkaloids are known with two indole groups. The number of known non-isoprenoid indole alkaloids is ... Indole alkaloids are a class of alkaloids containing a structural moiety of indole; many indole alkaloids also include isoprene ... Simple derivatives of indole Simple derivatives of β-carboline Pyrroloindole alkaloids Indole-3-carbinol Indole-3-acetic acid ... Pyrolo-indole alkaloids form a relatively small group of tryptamine derivatives. They are produced by methylation of indole ...
... NSC78580 5903-28-6 indole; tributylgermanium
Oxidation of indole by N-bromosuccinimide Cycloadditions of indole. Only the C-2 to C-3 pi-bond of indole is capable of ... Fischer indole synthesis. Main article: Fischer indole synthesis. The Fischer indole synthesis File:One-pot synthesis of ... Leimgruber-Batcho indole synthesis. Main article: Leimgruber-Batcho indole synthesis. The Leimgruber-Batcho indole synthesis ... Compounds that contain an indole ring are called indoles. The amino acid tryptophan is an indole derivative and the precursor ...
indole synonyms, indole pronunciation, indole translation, English dictionary definition of indole. n. 1. A white crystalline ... indole. Also found in: Medical, Legal, Encyclopedia, Wikipedia.. Related to indole: skatole, Isoquinoline, Indole test, Indole- ... indole. (ˈɪndəʊl) or indol. n. (Elements & Compounds) a white or yellowish crystalline heterocyclic compound extracted from ... In female rats, they discovered that a specific indole, known as indole-3-carbinol, significantly boosted the rate at which an ...
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FDAs Bacteriological Analytical Manual (BAM) presents the agencys preferred laboratory procedures for microbiological analyses of foods and cosmetics.
Indole was converted to 1H-indole-3-carbaldehyde in the presence of DMF, POCl3, NaOH. 1H-indole-3-carbaldehyde was taken and ...
... realizing dearomative arylcarboxylation of indoles with CO2. This strategy avoids common side reactions in transition-metal ... a visible light photoredox-catalyzed successive single electron transfer leading to dearomative arylcarboxylation of indoles ... Furthermore, 1-(2-bromophenethyl)-1H-indole-2-carboxylate and ethyl 1-(3-(2-bromophenyl)propyl)-1H-indole-2-carboxylate were ... which was much more significant than indole 1 (1.9) or the combination of indole 1 and Cs2CO3 (17.4). These results suggested ...
Information about 5-IT including basics, effects, dosage, history, legal status, photos, research, media coverage, and links to other resources.
Indole-3-carbinol, also called I3C, is a resulting compound that comes from eating vegetables such as Brussels sprouts, cabbage ... Busbee PB, Nagarkatti M, Nagarkatti PS. Natural indoles, indole-3-carbinol and 3,3-diindolymethane, inhibit T cell activation ... Busbee PB, Nagarkatti M, Nagarkatti PS. Natural indoles, indole-3-carbinol (I3C) and 3,3-diindolylmethane (DIM), attenuate ... Indole-3-carbinol and Tamoxifen cooperate to arrest the cell cycle of MCF-7 human breast cancer cells. Cancer Res 1999; 59:1244 ...
Here we investigate the impact of indole and 7HI on Pseudomonas aeruginosa PAO1 virulence and quorum sensing (QS)-regula … ... and many bacterial oxygenases readily convert indole to various oxidized compounds including 7-hydroxyindole (7HI). ... Indole is an extracellular biofilm signal for Escherichia coli, ... Indole and 7HI both altered extensively gene expression in a ... Indole is an extracellular biofilm signal for Escherichia coli, and many bacterial oxygenases readily convert indole to various ...
Indole analytical standard; CAS Number: 120-72-9; EC Number: 204-420-7; Synonyms: 1H-Benzo[b]pyrrole; find Supelco-442619 MSDS ... Indole may be used as an analytical reference standard for the determination of the analyte in teas, crab meat spoilages, ... Indole is classified under the volatile flavor compounds (VFCs). It is known to play significant role in various biological ...
This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2- ... N-(1-Methyl-1H-indol-5-yl)-N-(4-pyridinyl) carbamic acid methyl ester. A solution of methyl chloroformate (1.3 g) in 5 ml DCM ... Substituted pyridinylamino-1h-indoles,1h-indazoles,2h-indazoles, benzo (b)thiophenes and 1,2-benzisothiazoles. US 5185350 A ... 6. The compound as defined in claim 2 which is N-(1-methyl-1H-indol-5-yl)-N-(4-pyridinyl)-2-(carbamic acid, phenylmethyl ester) ...
Cruciferous veggies such as broccoli, cauliflower and more contain plant compounds that are important for optimal health, including chemoprotective compounds.
The effect of indole-3-carbinol (I3C), a major indolic metabolite in cruciferous vegetables, on lipopolysaccharide (LPS)- ... Antiangiogenic activity of indole-3-carbinol in endothelial cells stimulated with activated macrophages. *Wang M ... The effect of indole-3-carbinol (I3C), a major indolic metabolite in cruciferous vegetables, on lipopolysaccharide (LPS)- ...
Indol ställer ut i två montrar på pågående Nordbygg mässan som är nordens största bygg, VVS och värmepumps mässa. Monter A15:53 ... Indol ställer ut i två montrar på pågående Nordbygg mässan som är nordens största bygg, VVS och värmepumps mässa. Monter A15:53 ... Visar vi vårt sortiment av Indol varmvattenberedare. Vi har en inkopplad för att visa hur de faktiskt fungerar. Monter A27:41 ...
What is indoles? Meaning of indoles as a legal term. What does indoles mean in law? ... Definition of indoles in the Legal Dictionary - by Free online English dictionary and encyclopedia. ... Todo ello viene sintetizado en la expresion indole secular (Indoles saecularis).. La identidad de los cristianos laicos a la ... He continued the synthetic studies on indole alkaloids, added several new methodologies and new indole derivatives and ...
Ime indol je formirano od reči indigo i oleum, jer je indol prvi put izolovan tretmanom indigo boje oleumom. ... Indol je čvrst na sobnoj temperaturi. Indol mogu da proizvedu bakterije kao degradacioni produkt aminokiseline triptofana. On ... Indol i njegovi derivati takođe mogu biti sintetisani različitim metodama.[9][10][11] Glavni industrijski putevi počinju od ... Indol se često sreće u mirisima i lekovima. Jedinjenja koja sadrže indolni prsten se nazivaju indolima.[6] Indolna ...
... a selective synthetis of various indole derivatives. 3-Cyano-1H-indoles, 9H-pyrimido[4,5-b]indoles, or 9H-pyrido[2,3-b]indoles ... The resulting indoles can easily be transformed into other scaffolds, including 2,3- and 1,2-fused indoles, and indoles ... Utilizing this domino reaction and C-H functionalization at the indole C-3 position, polycyclic indoles were readily ... A one-pot synthesis of 3-bissulfonimido-indole derivatives directly from indoles, bissulfonimides, and (diacetoxyiodo)-2- ...
Nominated Substances: Indole. Nomination Date: 12/12/1990 Nominator: NASA Rationale: Lack of toxicological data; older studies indicate leukemogenic. NTP Principles: not specified More Detailed Information ...
  • Certain indole derivatives were important dyestuffs until the end of the 19th century. (
  • A number of indole derivatives have important cellular functions, including neurotransmitters such as serotonin. (
  • Indole and its derivatives can also be synthesized by a variety of methods. (
  • The latter include terpenoid structural elements, synthesized by living organisms from dimethylallyl pyrophosphate (DMAPP) and/or isopentenyl pyrophosphate (IPP): Non-isoprenoid: Simple derivatives of indole Simple derivatives of β-carboline Pyrroloindole alkaloids Indole-3-carbinol Indole-3-acetic acid Tryptamines Carbazoles Isoprenoid: hemiterpenoids: ergot alkaloids monoterpenoids. (
  • One of the simplest and yet widespread indole derivatives are the biogenic amines tryptamine and 5-hydroxytryptamine (serotonin). (
  • Pyrolo-indole alkaloids form a relatively small group of tryptamine derivatives. (
  • Synthesis and antiinflammatory activity of heterocyclic indole derivatives. (
  • He continued the synthetic studies on indole alkaloids, added several new methodologies and new indole derivatives and published dozens of research papers in this field of research during 1980-1988. (
  • Furthermore, fluoro -containing indole derivatives have received wide attention from either synthetic or pharmaceutical view for a long time due to their wide potential bioactivities [7-10]. (
  • Given the importance of heterocycle indole derivatives, much effort has been directed toward the development of methods for functionalization of the indole nucleus at N1 and C3 sites. (
  • Natural derivatives of aplysinopsin differ in the bromination pattern of the indole moiety ( Figure 1 ), variation in the structure of the C ring, including its oxidation state ( Figure 3 ) and number and position of N -methylation ( Figure 1 ), the presence and absence of the C-8-C-1′ double bond ( Figure 2 ), and the stereochemistry. (
  • Substituted indoles are structural elements of (and for some compounds, the synthetic precursors for) the tryptophan-derived tryptamine alkaloids, which includes the neurotransmitters serotonin and melatonin, as well as the naturally occurring psychedelic drugs dimethyltryptamine and psilocybin. (
  • Compounds that contain an indole ring are called indoles. (
  • Substituted indoles are structural elements of (and for some compounds the synthetic precursors for) the tryptophan-derived tryptamine alkaloids like the neurotransmitter serotonin , and melatonin . (
  • On day three, we found indole and putrescine, the main compounds that we were trying to detect," Jones says. (
  • Indole is an extracellular biofilm signal for Escherichia coli, and many bacterial oxygenases readily convert indole to various oxidized compounds including 7-hydroxyindole (7HI). (
  • Hence, indole-related compounds have potential as a novel antivirulence approach for the recalcitrant pathogen P. aeruginosa. (
  • Indole is classified under the volatile flavor compounds (VFCs). (
  • Odorous compounds including VFA, phenols and indoles were measured by gas chromatography (GC). (
  • This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). (
  • A range of substituted indoles are investigated as substrates, and thirteen new compounds have been synthesized. (
  • The indole scaffold is a prominent and privileged structural motif found in numerous natural products and various synthetic compounds. (
  • Here we focus on two of the compounds that can be derived from Trp: IAA and indole glucosinolates. (
  • Indole glucosinolates are members of the glucosinolate family (mustard seed oils) of compounds found in Brassica species ( 1 , 10 , 11 ). (
  • A huge diversity of indole alkaloids are frequently found in marine invertebrates and they have been considered lead compounds for the discovery of new drugs in medicinal chemistry [ 9 , 12 ]. (
  • When the double bond is present, the formula I compounds represent indoles. (
  • The Leimgruber-Batcho indole synthesis is an efficient method of synthesizing indole and substituted indoles. (
  • One of the oldest and most reliable methods for synthesizing substituted indoles is the Fischer indole synthesis, developed in 1883 by Emil Fischer. (
  • Although the synthesis of indole itself is problematic using the Fischer indole synthesis, it is often used to generate indoles substituted in the 2- and/or 3-positions. (
  • Indole can still be synthesized, however, using the Fischer indole synthesis by reacting phenylhydrazine with pyruvic acid followed by decarboxylation of the formed indole-2-carboxylic acid. (
  • Bartoli indole synthesis Bischler-Möhlau indole synthesis Cadogan-Sundberg indole synthesis Fukuyama indole synthesis Gassman indole synthesis Hemetsberger indole synthesis Larock indole synthesis Madelung synthesis Nenitzescu indole synthesis Reissert indole synthesis Baeyer-Emmerling indole synthesis In the Diels-Reese reaction dimethyl acetylenedicarboxylate reacts with 1,2-diphenylhydrazine to an adduct, which in xylene gives dimethyl indole-2,3-dicarboxylate and aniline. (
  • Due to this activity, it is not surprising that the indole ring system has become an important building block or intermediate in the synthesis of many pharmaceutical agents. (
  • 1 Application of Pd-Catalyzed Annulation to the Synthesis of the Indole Acetic Acid. (
  • Phosphorylated indoles are widely used not only in pharmaceutical chemistry, but also in the field of fine organic synthesis and materials science. (
  • Indole-7-carboxylic acid is an important raw material and intermediate used in organic synthesis, pharmaceuticals, agrochemicals and dyestuff fields. (
  • The most recent advances on catalytic methods to achieve the synthesis of substituted indole are highlighted herein. (
  • have reported on a one-pot, three-component procedure for the synthesis of 2,3-substituted indoles based on Cacchi s protocol (Scheme 1). (
  • Scheme 3 - Synthesis of 2,3-disubstituted indoles using a Pd-catalyzed C-N/C-C coupling strategy. (
  • Synthesis and pharmacology of N-(pyridyalkyl)indoline and indoles" CA 70:19857, 1968. (
  • Indole-3-carbonitrile is used as a synthesis reagent for preparation of 4-substituted β-lactams, biologically active indoles, inhibitors of glycogen synthase kinase 3β (GSK-3), indole fragments as inosine monophosphate dehydrogenase (IMPDH) inhibitors and HIV-1 integrase inhibitors. (
  • It is also used as a reactant for intramolecular oxidative C-H coupling reactions with applications in medium-ring synthesis techniques and for preparation of tryptophan dioxygenase inhibitors pyridyl-ethenyl-indoles as potential anticancer immunomodulators. (
  • Attia, M.I. Synthesis, Spectroscopic Characterization and Antimicrobial Potential of Certain New Isatin-Indole Molecular Hybrids. (
  • In the 1930s, interest in indole intensified when it became known that the indole substituent is present in many important alkaloids (e.g., tryptophan and auxins), and it remains an active area of research today. (
  • many indole alkaloids also include isoprene groups and are thus called terpene indole or secologanin tryptamine alkaloids. (
  • The amino acid tryptophan is the biochemical precursor of indole alkaloids. (
  • The action of some indole alkaloids has been known for ages. (
  • Some 200 dimeric indole alkaloids are known with two indole groups. (
  • The number of known non-isoprenoid indole alkaloids is small compared to the number of indole alkaloids. (
  • The tryptamine skeleton is part of the vast majority of indole alkaloids. (
  • Some simple indole alkaloids do not contain tryptamine, such as gramine and glycozoline (the latter is a derivative of carbazole). (
  • Isoprenoid indole alkaloids include residues of tryptophan or tryptamine and isoprenoid building blocks derived from the dimethylallyl pyrophosphate and isopentenyl pyrophosphate. (
  • Ergot alkaloids are a class of hemiterpenoid indole alkaloids related to lysergic acid, which, in turn, is formed in a multistage reactions involving tryptophan and DMAPP. (
  • The proposal aims at addressing the collective syntheses of a series of bioactive indole alkaloids (strictamine, aspidophylline A and alsmaphorazine C) from a common intermediate. (
  • Voafinidine and voalenine, a novel indoles of the aspidosperma alkaloids from Tabernaemontana. (
  • This review discusses the isolation, structural elucidation, and biological activities of halogenated indole alkaloids obtained from marine invertebrates. (
  • A compilation of the 13 C-NMR spectral data of these selected natural indole alkaloids is also provided. (
  • The biological activity of marine indole alkaloids is clearly a product of the unique functionality and elements involved in the biosynthesis of marine natural products. (
  • In female rats, they discovered that a specific indole , known as indole -3-carbinol, significantly boosted the rate at which an enzyme converted a form of estrogen to 2-hydroxyestrone, an inactive version that doesn't trigger mammary tumor growth. (
  • Indole 3-carbinol has cancer-preventive effects, but it has not been shown to treat cancer in humans. (
  • Laboratory and animal studies suggest that indole-3-carbinol may prevent a variety of cancers, including estrogen-dependent cancers, but only one clinical trial has been performed. (
  • Indole-3-carbinol is formed when these vegetables are cut, chewed or cooked. (
  • People use indole-3-carbinol for cancer prevention, to treat systemic lupus erythematosus (SLE), and for many other conditions, but there is no good scientific evidence to support these uses. (
  • There is interest in indole-3-carbinol for cancer prevention, particularly breast, cervical, and colon cancer, because diets with higher amounts of fruits and vegetables are linked to a decreased risk of these cancers. (
  • Indole-3-carbinol is present in several vegetables and might help protect against cancer. (
  • Early research shows that taking indole-3-carbinol by mouth helps treat cervical dysplasia. (
  • Early research shows that taking indole-3-carbinol by mouth might reduce the size of these lesions and improve symptoms in some women with this condition. (
  • Early research shows that taking indole-3-carbinol along with standard chemotherapy and surgery allows women with ovarian cancer to live longer , and increases the time that they stay cancer-free. (
  • There is some evidence that long-term use of indole-3-carbinol might reduce the wart -like growths in people with recurrent respiratory papillomatosis. (
  • Early research shows that taking indole-3-carbinol by mouth does not improve symptoms of SLE. (
  • More evidence is needed to rate the effectiveness of indole-3-carbinol for these uses. (
  • Indole-3-carbinol is POSSIBLY SAFE for most people when taken as a medicine under proper medical supervision. (
  • In higher doses, indole-3-carbinol can cause balance problems, tremor, and nausea . (
  • There isn't enough reliable information to know if indole-3-carbinol is safe to use when pregnant or breast-feeding. (
  • Indole-3-carbinol might slow blood clotting. (
  • In theory, taking indole-3-carbinol might increase the risk of bleeding in people with bleeding disorders . (
  • In theory, taking indole-3-carbinol might cause bleeding complications during surgery. (
  • Stop taking indole-3-carbinol at least 2 weeks before surgery. (
  • Indole-3-carbinol might increase how quickly the liver breaks down some medications. (
  • I need to find out if Indole 3 Carbinol is bad to take if I am hypothyroid! (
  • Indole-3 carbinol may be beneficial in the treatment of systemic lupus erythematosus. (
  • Anti-cancer and cardioprotective effects of indol-3-carbinol in doxorubicin-treated mice. (
  • Antiobesity activities of indole-3-carbinol in high-fat-diet-induced obese mice. (
  • Attenuation of hyperglycemia-mediated oxidative stress by indole-3-carbinol and its metabolite 3, 3'- diindolylmethane. (
  • Both indole-3-carbinol and myo-inositol inhibit the development of vinyl carbamate induced pulmonary adenocarcinoma in mice. (
  • Enhanced inhibition of lung adenocarcinoma by combinatorial treatment with indole-3-carbinol and silibinin. (
  • Immunoregulatory effects of indole-3-carbinol on monocyte-derived macrophages in systemic lupus erythematosus. (
  • In vivo pharmacodynamics of indole-3-carbinol in the inhibition of prostate cancer in transgenic adenocarcinoma. (
  • Indole-3-carbinol (I3C), a naturally occurring compound found in vegetables of the Brassica genus, such as broccoli and cabbage, is a promising anticancer agent previously shown to induce a G(1) cell-cycle arrest in the cells of human lymph node carcinoma of prostate (LNCaP) through regulation of specific G(1)-acting cell-cycle components. (
  • Indole-3-carbinol inhibition of androgen receptor expression and downregulation of androgen responsiveness in human prostate cancer cells. (
  • Dietary indoles including indole-3-carbinol (I3C) found in cruciferous vegetables such as cauliflower, cabbage and Brussels sprouts, as well as its derivative, diindolylmethane (DIM) have also been known for their health benefits and for their anti-cancer properties. (
  • Combinations of indole-3-carbinol and silibinin suppress inflammation-driven mouse lung tumorigenesis by modulating critical cell cycle regulators. (
  • We studied the efficacy of combinations of indole-3-carbinol (I3C) and silibinin (Sil), 20µmol/g diet each, against mouse lung tumors induced by 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) and driven by lipopolysaccharide (LPS), a potent inflammatory agent and constituent of tobacco smoke. (
  • Indole-3-carbinol (I3C), a naturally occurring component of Brassica vegetables such as cabbage, broccoli, and Brussels sprouts, has been shown to reduce the incidence of spontaneous and carcinogen-induced mammary tumors. (
  • Indole-3-carbinol inhibits the expression of cyclin-dependent kinase-6 and induces a G1 cell cycle arrest of human breast cancer cells independent of estrogen receptor signaling. (
  • Indole-3-carbinol (I3C), a chemical found in vegetables of the broccoli family, is thought to possess cancer preventive properties. (
  • What Is the Scientific Evidence for Indole-3-Carbinol? (
  • Chemopreventive Properties of Indole-3-Carbinol, Diindolylmethane and Other Constitents of Cardamom Against Carcinogenesis. (
  • I was thinking of increasing the Indoplex to 240mg and possibly trying indole-3-carbinol. (
  • Will the indole-3-carbinol be more effective than the Indoplex? (
  • Indole-3-Carbinol after 11oxo when starting 6oxo? (
  • Indole-3-Carbinol (I3C) as part of PCT? (
  • Determine the maximum tolerated dose of indole-3-carbinol in healthy participants. (
  • Arm I: Participants receive a single dose of oral indole-3-carbinol on day 1. (
  • Cohorts of 3 participants receive escalating doses of indole-3-carbinol until the maximum tolerated dose (MTD) is determined. (
  • Indole-3-Carbinol Assay data Indole-3-Carbinol 99.0% min. (
  • Computer model of a molecule of indole-3-carbinol (I3C), a powerful antioxidant found in vegetables of the cabbage family (cruciferous family). (
  • Indole Plus provides the clinically recommended amount of stabilized Indole-3-Carbinol with a unique delivery system that maximizes the absorption and utilization of I3C. (
  • An enzymatic cyclopentyl[b]indole formation involved in scytonemin biosynthesis. (
  • The addition of indole at 30 degrees C compared to 37 degrees C most significantly repressed genes involved in uridine monophosphate (UMP) biosynthesis (carAB, pyrLBI, pyrC, pyrD, pyrF and upp) and uracil transport (uraA). (
  • In Trp-independent IAA biosynthesis, indole-3-glycerol phosphate or indole is the likely precursor but little is known about the biochemical pathway to IAA. (
  • Taken together, our data suggest a model in which CYP79B2 and CYP79B3 metabolize Trp to IAOx that can be used for either IAA or indole glucosinolate biosynthesis. (
  • Additionally, these packets also contain phytonutrients such as sulforaphane and indoles (in cruciferous vegetables) and ellagic acid (in strawberries), which promote healthy cell function and development. (
  • The amino acid tryptophan is an indole derivative and the precursor of the neurotransmitter serotonin. (
  • When indole is needed in the cell, it is usually produced from tryptophan by tryptophanase. (
  • Indole can be produced by bacteria as a degradation product of the amino acid tryptophan . (
  • Indole is produced via anthranilate and is alkylated to give the amino acid tryptophan. (
  • Indeed, their studies showed, chemicals that posses a structure known as an indole ring -- including the essential amino acids L-tryptophan and L-proline -- provide "a more specific means of lowering the formation of mutagens" than had the antioxidants. (
  • ScyB, a leucine dehydrogenase homolog, converts L-tryptophan to indole-3 pyruvic acid ( 3 ). (
  • Tryptophan (Trp) and its indolic precursors are the sources of indole-3-acetic acid (IAA), certain glucosinolates, and phytoalexins ( 3 ). (
  • Så, i 1866 reduserte Adolf von Baeyer oxindol til indol ved hjelp av sinkstøv . (
  • Then, in 1866, Adolf von Baeyer reduced oxindole to indole using zinc dust. (
  • Indole itself was first obtained by Adolf von Baeyer in 1866 while decomposing Indigo. (
  • i ) the indole-3-acetonitrile (IAN) pathway [Trp → indole-3-acetaldoxime (IAOx) → IAN → IAA] and ( ii ) the indole pyruvic acid (IPA) pathway (Trp → IPA → indole-3-acetaldehyde → IAA) ( 4 ). (
  • Indole is an aromatic heterocyclic organic compound with formula C8H7N. (
  • Indoles, dihydroisoquinolines, and dihydroquinolines were efficiently prepared by ruthenium-catalyzed heterocyclizations of aromatic homo- and bis-homopropargyl amines or amides in the presence of pyridine. (
  • Indole is an aromatic molecule with diverse signalling roles. (
  • Indole is an aromatic molecule produced by over 85 species of bacteria with multiple and diverse signalling roles 5 . (
  • Investigators previously reported that the heterocyclic aromatic amine 2-amino-9H-pyrido[2,3-b]indole (AαC) -- the most abundant aromatic amine carcinogen formed in tobacco smoke and a rodent GI genotoxicant -- is present in the urine of tobacco smokers in a dose-dependent manner but is absent in the urine of nonsmokers. (
  • Subsequently, the development of efficient methods that allow rapid access to functionalized indoles with different substitution patterns (at C-2, C-3, N-atom and aromatic ring, Figure 1) constitutes an emerging area. (
  • "3-Indolyl-1-naphthylmethanes: new cannabimimetic indoles provide evidence for aromatic stacking interactions with the CB(1) cannabinoid receptor" Bioorg Med Chem . (
  • Molecular modeling and receptor docking studies of naphthoylindole 16, its 2-methyl congener (19) and indolyl-1-naphthylmethanes 11 and 14, combined with the receptor affinities of these cannabimimetic indoles, strongly suggest that these cannabinoid receptor ligands bind primarily by aromatic stacking interactions in the transmembrane helix 3-4-5-6 region of the CB(1) receptor. (
  • There is some evidence that the indoles bind to a somewhat different site on the receptor than traditional cannabinoids, and interact with the receptor primarily by aromatic stacking. (
  • The molecule occupies a crystallographic inversion center and consists of two 3-substituted 1 H -indole moieties linked by a (1E,2E)-1,2-dimethylenehydrazine bridge, one of numerous examples in which two aromatic ring systems are joined by this 4-atom bridge. (
  • The indole subunit is a near-ubiquitous component of biologically active natural products, and its study has been a major focus of research for generations. (
  • Nitrogen-containing heterocycles, including 1 H -indoles and electron-deficient 1 H -pyrroles, undergo a smoth and mild palladium/norbornene-cocatalyzed regioselective alkylation with primary alkyl bromides at the C-H bond adjacent to the NH group to give 2-alkyl-1 H -indoles and 2-substituted or 2,3-disubstituted 5-alkyl-1 H -pyrroles in good yields. (
  • The catalytic system showed high catalytic activity for the methylation of C-H bonds in aryl alkyl ketones, aryl acetonitriles, and indoles, with wide substrate scope and good functional group tolerance. (
  • [1] It condenses with serine via Michael addition of indole to PLP-aminoacrylate . (
  • Bulky, electron-rich phosphines as the supporting ligand in combination with Pd 2 (dba) 3 enable N -arylation of indoles with aryl iodides, bromides, chlorides, and triflates. (
  • The last part of the thesis (Project IV) describes a C-2 selective arylation of indoles where diaryliodonium salts were used in combination with hetero-geneous palladium catalysis. (
  • Direct palladium-catalyzed C-2 and C-3 arylation of indoles: a mechanistic rationale for regioselectivity. (
  • We have recently developed palladium-catalyzed methods for direct arylation of indoles (and other azoles) wherein high C-2 selectivity was observed for both free (NH)-indole and (NR)-indole. (
  • Indole is widely distributed in the natural environment and can be produced by a variety of bacteria. (
  • Lowering levels of toxic by-products: Harmful bacteria can produce toxins, such as indole , skatole, and methane because of their metabolic reaction to certain foods. (
  • But when it accompanies 200 ppm of indole (half of that haxane's bacteria-inhibiting dose), a mere 6. (
  • This study suggests Tyrian purple indole precursors could be obtained from opportunistic ubiquitous bacteria. (
  • brasilense cepa SP7 inducen a que la bacteria utilice varias rutas metabolicas para la sintesis de indoles y, en especial, AIA a partir del TRP. (
  • Indole signalling in bacteria can be divided into two main types: persistent signalling and pulse signalling. (
  • 3. The compound as defined in claim 2 which is 1-methyl-5-(propyl-4-pyridinylamino)-1H-indole. (
  • 6. The compound as defined in claim 2 which is N-(1-methyl-1H-indol-5-yl)-N-(4-pyridinyl)-2-(carbamic acid, phenylmethyl ester)acetamide hydrochloride. (
  • The title compound, C 27 H 22 N 2 O 2 , was synthesized by the reaction of indole-3-carb-aldehyde with 4-methoxyaceto-phenone and ammonium acetate in glycol under microwave irradiation. (
  • I don't know of any way of removing indole from an existing compound that wouldn't also remove other necessary aroma molecules that you'd want to keep. (
  • The title compound, C 34 H 30 N 4 O 2 , lies on an inversion center and consists of two 3-substituted-1 H -indole units linked by a 1,2-dimethyl-enehydrazine bridge. (
  • In this report we disclose the discovery that ScyC (NpR1274), an enzyme encoded by the scytonemin cluster, catalyzes cyclization and decarboxylation of ScyA product 2 to form ketone 5 , thereby constructing the indole-fused cyclopentane moiety of the natural product. (
  • Oxindole-3-acetic acid (OxIAA), OxIAA conjugated to a hexose moiety via the carboxyl group, and the conjugates indole-3-acetyl aspartic acid (IAAsp) and indole-3-acetyl glutamate (IAGlu) were identified by mass spectrometry as primary products of IAA fed to the plants. (
  • Indole cell signaling occurs primarily at low temperatures in Escherichia coli. (
  • We have shown that the quorum-sensing signals acylhomoserine lactones, autoinducer-2 (AI-2) and indole influence the biofilm formation of Escherichia coli. (
  • Here we demonstrate that indole plays a critical role in the regulation of the cytoplasmic pH of Escherichia coli . (
  • On the basis of a proposed pharmacophore for the cannabimimetic indoles, a series of pyrroles and indenes were developed, some of which are potent cannabinoids. (
  • Two groups have described cannabimimetic indenes, which have been employed as rigid models for the receptor interactions of cannabimimetic indoles with the CB1 receptor. (
  • Reaction of aniline and ethylene glycol to give indole. (
  • Other precursors to indole include formyltoluidine, 2-ethylaniline, and 2-(2-nitrophenyl)ethanol, all of which undergo cyclizations. (
  • In 1869, he proposed a formula for indole (left). (
  • The correct structural formula of strychnine was determined only in 1947, although the presence of the indole nucleus in the structure of strychnine was established somewhat earlier. (
  • Indole is a common component of fragrances and the precursor to many pharmaceuticals. (
  • We have identified two Arabidopsis cytochrome P450s (CYP79B2 and CYP79B3) that can convert Trp to indole-3-acetaldoxime (IAOx), a precursor to IAA and indole glucosinolates. (
  • Il s'agit d'une source d'informations unique sur les substances chimiques fabriquées et importées en Europe. (
  • [1] I 1869 foreslo han formelen til indol (til venstre) som i dag er akseptert. (
  • Indol je aromatično heterociklično organsko jedinjenje . (
  • Indol-5,6-hinon je organsko jedinjenje , koje sadrži 8 atoma ugljenika i ima molekulsku masu od 147,131 Da . (
  • Indole chemistry began to develop with the study of the dye indigo. (
  • Indole undergoes electrophilic substitution, mainly at position 3 (see diagram in right margin). (
  • Indole undergoes electrophilic substitution , mainly at position 3. (
  • The mechanism of the iodination step is proposed to proceed via a Cu( III )-iodide species that undergoes electrophilic addition at the C3 position of the indole motif. (
  • On the basis of these findings, a mechanistic interpretation is presented that features an electrophilic palladation of indole, accompanied by a 1,2-migration of an intermediate palladium species. (
  • A transition-metal/quinone complex is an effective catalyst for aerobic dehydrogenation of 3 indolines to the corresponding indoles. (
  • In a regioselective dehydrogenative alkylation of indolines using readily available alcohols as the alkylating reagents, a single air- and moisture-stable manganese catalyst provides access to either C3- or N-alkylated indoles depending on the solvent used. (
  • The metabolism of indole-3-acetic acid (IAA) was investigated in 14-d-old Arabidopsis plants grown in liquid culture. (
  • Recently we discovered two allosteric modulators 1 and 2 for the G protein -coupled receptor GPRC6A incorporating the privileged 2-phenyl-indole scaffold, functionalised at the 3-position. (
  • Scheme 1 - One-pot, three-component procedure for accessing the 2,3-substituted indole scaffold. (
  • Notably, sprouts of many broccoli cultivars contain negligible quantities of indole glucosinolates, which predominate in the mature vegetable and may give rise to degradation products (e. (
  • We show in biofilms that indole addition leads to more extensive differential gene expression at 30 degrees C (186 genes) than at 37 degrees C (59 genes), that indole reduces biofilm formation (without affecting growth) more significantly at 25 and 30 degrees C than at 37 degrees C and that the effect is associated with the quorum-sensing protein SdiA. (
  • Immunoblot and quantitative RT-PCR assays revealed that I3C inhibited the expression of AR protein and mRNA levels within 12 h of indole treatment. (
  • A one-pot selective N -alkylation of unprotected indoles with alcohols and TsCl is also realized. (
  • The developed protocol is highly C-2 selective and tolerates structural variations both in the indole and in the diaryliodonium salt. (
  • Investigation of these indoles led to the discovery of a CB2 selective ligand, 3- (1-naphthoyl)-N-propylindole. (
  • Subsequent work has provided several additional CB2 selective indoles. (
  • Deltakelsen av et enslig elektronpar av nitrogen i den aromatiske ringen medfører at indol ikke er en base , og det oppfører seg ikke som et usammensatt amin . (
  • In addition, indole affected the utilization of carbon, nitrogen and phosphorus, and 7HI abolished swarming motility. (
  • Due to the poor nucleophilicity of the nitrogen atom of indoles and the competing alkylation reaction at the C-3 position, the use of more sterically hindered ketones with a lower electrophilicity as N -alkylation reagents has been a great challenge. (
  • We have made an exciting observation that dietary indoles such as DIM can completely suppress the clinical disease in an experimental model of MS known as Experimental Autoimmune Encephalomyelitis (EAE). (
  • The I3C-mediated cell cycle arrest and repression of CDK6 production were also observed in estrogen receptor-deficient MDA-MB-231 human breast cancer cells, which demonstrates that this indole can suppress the growth of mammary tumor cells independent of estrogen receptor signaling. (
  • En av de eldste og mest pålitelige metoder for å syntetisere substituerte indoler er Fischer indolsyntese som ble utviklet i 1883 av Emil Fischer . (
  • Selv om syntesen av indol selv er problematisk med bruk av Fischer indolsyntese, blir den ofte brukt til å generere indolsubstitutter i 2- og/eller 3-posisjonene. (
  • A consecutive detosylation/alkylation transformation of tosylated indoles and phenols with alkoxides/alcohols as the alkylation reagents features mild reaction conditions, high ipso -selectivity, and good functional group tolerance. (
  • An efficient and cost-effective copper-mediated aerobic oxidative C-H iodination and nitration of indoles via double C-H functionalization is reported. (
  • These uracil-related genes are also repressed at 30 degrees C by SdiA, which confirms SdiA is involved in indole signaling. (
  • Camalexin is a simple indole alkaloid produced by the plant Arabidopsis thaliana, often used as a model for plant biology. (
  • In order to develop new potential GPRC6A ligands we engaged in the development of synthetic routes to provide 2-phenyl-indoles with a variety of substituents at the indole 3-position. (
  • The strategy reported by the authors showed a wide range of applicability in terms of substituents, in particular for the challenging 4-substituted indoles. (
  • H indoles and N -protected indoles with ortho -substituted, electron-rich, electron-deficient, or halogenated diaryliodonium salts were achieved to give the desired products in high to excellent isolated yields within 6 to 15 h at room temperature or 40 °C. (
  • New isatin-indole molecular hybrids 5a - n have been synthesized and characterized by various spectroscopic tools. (
  • Moreover, the authors expanded the reaction scope to obtain 1,2,3-trisubstituted indoles by switching the order of addition of the two boronic acids. (
  • In examining the presence of indole-3-acetic acid (IAA) in supernatants of pink-pigmented facultativemethylotrophic (PPFMs) bacterial cultures, three out of the 16 isolates tested showed a positive reaction ina colorimetric assay. (
  • The reaction order was determined for iodobenzene (zero order), indole (first order), and the catalyst (first order). (
  • In case of free (NH)-indole, regioselectivity of the arylation reaction (C-2 versus C-3) was achieved by the choice of magnesium base. (