Indole derivatives interact with DOPC in Langmuir...
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 ...
Studies On Developing A Facile Route For The Synthesis Of Highly Substituted Quinoline And Indole Derivatives
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 ...
EP 1100780 A1 20010523 - 2,3,3a,4,9,9a-HEXAHYDRO-8-HYDROXY-1H-BENZ[F]INDOLES, A METHOD FOR THE PRODUCTION THEREOF, AND THEIR...
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).
Prospects of Indole derivatives as methyl transfer inhibitors: antimicrobial resistance managers | BMC Pharmacology and...
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
AZA)INDOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - Patent application
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 ...
Catechol and indole derivatives in a transplantable islet-cell tumour of the golden hamster. - Semantic Scholar
Semantic Scholar extracted view of Catechol and indole derivatives in a transplantable islet-cell tumour of the golden hamster. by Lennart Cegrell et al.
COMPOUND INCLUDING INDOLE DERIVATIVE, ORGANIC ELECTRONIC ELEMENT USING SAME, AND TERMINAL THEREOF - Patent application
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 ...
KAKEN - Research Projects | Novel synthesis of indole derivatives based on the palladium catalyzed cross-coupling reaction with...
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
Indole Derivatives - AMINO ACIDS - Products
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WO2008101995 INDOLE DERIVATIVES
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.
Inhibition of growth factor-induced Ras signaling in vascular endothelial cells and angiogenesis by 3,3′-diindolylmethane :...
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 ...
Synthesis, ligand binding, QSAR, and CoMFA study of 3 beta-(p-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters |...
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.
Molecules | Free Full-Text | Platinum-Catalyzed Allylation of 2,3-Disubstituted Indoles with Allylic Acetates
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.
Excitation and Excited State Properties of Heterocyclic Chromophores. Indole and Purine Derivatives of Biological Significance
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
US Patent for Derivatives of 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid Patent (Patent # 4,070,371 issued January 24,...
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.
Description: Biochemical investigations on bacterial and fungal dimethylallyltryptophan synthases
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 ...
سعر وملعومات Indomethacin 25mg 24 caps
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Browsing Student Research, Projects and Publications by Author Bohorquez, Maria
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 ...
Diindolylmethane Derivatives as Apoptosis Inductors in L5178y Cells
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 H-NMR | C-NMR Spectral Analysis NMR Spectrum
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.
A survey of core replacements in indole-based HIV-1 attachment inhibitors<...
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 ...
Patente US4141880 - Flame retarded nylon composition - Google Patentes
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 - How does it Work for Estrogen Levels?
Diindolylmethane Benefits as an Estrogen Blocking Supplement & Testosterone Booster. Effects on Weight Loss, Bodybuilding, PMS, Menopause, Cancer & More.
Diindolylmethane: Healthy Hormone Balance For Men & Women?
Diindolylmethane is suggested to balance levels of estrogen, creating a healthy hormone balance for both men and women. Effects can relieve...
Gentaur Molecular :Gene Link \ 5 Nitroindole 200 nmol scale \ 26-6476-02
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Trandolapril Cas number 87679-37-6, Trandolapril exporters, Trandolapril manufacturers,Trandolapril suppliers,Trandolapril...
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
Molecules | Free Full-Text | Synthesis and Evaluation of Novel α-Aminoamides Containing an Indole Moiety for the Treatment of...
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 | Horizon Health Shop
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 - PubChem
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.
4-Azaindole | CAS 272-49-1 | SCBT - Santa Cruz Biotechnology
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 - PubChem
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,...
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...
First synthesis of 6,7-diaminoindole and 1,2,5-selenadiazolo[3,4-g]indole
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%
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Alfa Aesar™ 3-(1-Piperazinylmethyl)indole, 95% 1g Alfa Aesar™ 3-(1-Piperazinylmethyl)indole, 95%
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2,3-dihydro-1H-indol-5-amine,dihydrochloride 2759-14-0 MSDS, Safety Technical Specifications MSDS
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.
Diindolylmethane - Scientific Review on Usage, Dosage, Side Effects | Examine.com
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.
ChemIDplus - 55142-77-3 - PJYCVBMPEOJLKW-UHFFFAOYSA-N - Indole-3-carboxamide, N-(2-(hydroxy(3-indolyl)methylthio)ethyl)- -...
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.
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Buy DIM Diindolylmethane Capsules - Balance Hormones
Buy DIM Diindolymethane Capsules. DIM Diindolymethane aids healthy estrogen metabolism and helps balance hormones for men and women. We offer it for only...
2-[(E)-3-(3,3-Dimethyl-1-phenyl-1,3-dihydro-2H-indol-2-ylidene)-1-propenyl]-3,3-dimethyl-1-phenyl-3H-indolium chloride - Alfa...
Alfa Chemistry is the worlds leading provider for special chemicals. We offer qualified products for 122295-58-3(2-[(E)-3-(3,3-Dimethyl-1-phenyl-1,3-dihydro-2H-indol-2-ylidene)-1-propenyl]-3,3-dimethyl-1-phenyl-3H-indolium chloride),please inquire us for 122295-58-3(2-[(E)-3-(3,3-Dimethyl-1-phenyl-1,3-dihydro-2H-indol-2-ylidene)-1-propenyl]-3,3-dimethyl-1-phenyl-3H-indolium chloride).
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Indole Derivatives Isolated from Brown Alga Sargassum thunbergii Inhibit Adipogenesis through AMPK Activation in 3T3-L1...
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.
Bioactive Heterocycles V by Nurullah Saracoglu (auth.), Mahmud Tareq Hassan Khan (eds.) - A Bike Life Book Archive
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 ...
The metabolism of some 1-hydroxylated indoles in the rat. - Semantic Scholar
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.
Trikentramides A-D: Indole Alkaloids from the Australian Sponge Trikentrion flabelliforme
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 ...
Identification of Novel 5-hydroxy-1H-indole-3-carboxylates with Anti-HBV Activities Based on 3D-QSAR Studies - Certara
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
Design of a thermally controlled sequence of triazolinedione-based click and transclick reactions
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 ...
Molecular docking and spatial coarse graining simulations as tools to investigate substrate recognition, enhancer binding and...
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 ...
Four Fatalities Involving 5-IT<...
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 ...
Publikationen: Leibniz-Institut für Pflanzenbiochemie
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 ...
Plus it
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 ...
CCCC 1962, Volume 27, Issue 5, Abstracts pp. 1278-1283 | Collection of Czechoslovak Chemical Communications
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 ...
Temozolomide and Sunitinib Malate in Treating Patients With Stage III or Stage IV Malignant Melanoma - Tabular View -...
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.. ...
Perifosine + Sunitinib Malate for Patients With Advanced Cancers - Tabular View - ClinicalTrials.gov
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 | Sutent® (sunitinib malate) - The Max Foundation
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 - Wikipedia
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 ...
Leicester Research Archive: Physiological modeling of formulated and crystalline 3,3-diindolylmethane pharmacokinetics...
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 ...
Effects of HDM2 antagonism on sunitinib resistance, p53 activation, SDF-1 induction, and tumor infiltration by CD11b+/Gr-1+...
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-Diindolylmethane
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) confers protection against ionizing radiation by a unique mechanism
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 …
Buy Diindolylmethane 1kg Brain Health Provider - Bionootropics
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.
Diindolylmethane found in vegetables and soy slow cancer cell growth - Nutrition Express Articles
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: ...
Regiospecific synthesis of 2,3-disubstituted indoles from isatins [PeerJ Preprints]
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
Plus it
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 ...
DIM (Diindolylmethane) 150 mg
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 ...
Indole-3-Carbinol (I3C), What is Indole-3-Carbinol, What is it made from, what other names does it have.
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 p | Open-i
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 - Natures Way - DIM-Plus 120vcap
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
2-Acetone, condensation product with phenol - Dossier Evaluation status - ECHA
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 - Wikipedia
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 ...
2-Acetone, condensation product with phenol - Registration Dossier - ECHA
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 ...
2-Acetone, condensation product with phenol - Registration Dossier - ECHA
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 ...
2-Acetone, condensation product with phenol - Registration Dossier - ECHA
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 ...
2-Acetone, condensation product with phenol - Registration Dossier - ECHA
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 ...
Condensation products of triethanolamine with... - Registration Dossier - ECHA
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 ...
China Indole 3 Carbinol Powder Manufacturers, Suppliers - Wholesale Bulk Indole 3 Carbinol Powder in Stock - Unipharmpro
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 >= 98 % | 144110-43-0 | Sigma...
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;
Study Of Sunitinib Plus FOLFOX In Patients With Solid Tumors
This study determined the maximum tolerated dose and safety of SU011248 (sunitinib malate,
SUTENT) in combination with FOLFOX [Leucovorin + Fluorouracil
3,3-Diindolylmethane - wikidoc
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, BSA conjugated
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
Source Naturals, DIM (Diindolylmethane), 100 mg, 60 Tablets | The Supplement Shop
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
The new psychoactive substances 5-(2-aminopropyl)indole (5-IT) and 6-(2-aminopropyl)indole (6-IT) interact with monoamine...
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.