Quinazolines. Medical search

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A publication issued at stated, more or less regular, intervals.

"The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.

The premier bibliographic database of the NATIONAL LIBRARY OF MEDICINE. MEDLINE® (MEDLARS Online) is the primary subset of PUBMED and can be searched on NLM's Web site in PubMed or the NLM Gateway. MEDLINE references are indexed with MEDICAL SUBJECT HEADINGS (MeSH).

Publications in any medium issued in successive parts bearing numerical or chronological designations and intended to be continued indefinitely. (ALA Glossary of Library and Information Science, 1983, p203)

Cell membrane glycoproteins that are selectively permeable to potassium ions. At least eight major groups of K channels exist and they are made up of dozens of different subunits.

Gated, ion-selective glycoproteins that traverse membranes. The stimulus for ION CHANNEL GATING can be due to a variety of stimuli such as LIGANDS, a TRANSMEMBRANE POTENTIAL DIFFERENCE, mechanical deformation or through INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS.

The opening and closing of ion channels due to a stimulus. The stimulus can be a change in membrane potential (voltage-gated), drugs or chemical transmitters (ligand-gated), or a mechanical deformation. Gating is thought to involve conformational changes of the ion channel which alters selective permeability.

An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.

Potassium channel whose permeability to ions is extremely sensitive to the transmembrane potential difference. The opening of these channels is induced by the membrane depolarization of the ACTION POTENTIAL.

A family of DNA plant viruses that infect eukaryotic algae.

Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).

A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.

A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.

A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.

A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN RECEPTOR AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.

Any chemical species which accepts an electron-pair from a LEWIS BASE in a chemical bonding reaction.

Chemicals with two conjoined aromatic rings incorporating two nitrogen atoms and one of the carbons oxidized with a keto oxygen.

Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)

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 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.

Scandium. An element of the rare earth family of metals. It has the atomic symbol Sc, atomic number 21, and atomic weight 45.

Compounds with a benzene ring fused to a thiazole ring.

Substances that sweeten food, beverages, medications, etc., such as sugar, saccharine or other low-calorie synthetic products. (From Random House Unabridged Dictionary, 2d ed)

Flavoring agent and non-nutritive sweetener.

Inhibitors of the enzyme, dihydrofolate reductase (TETRAHYDROFOLATE DEHYDROGENASE), which converts dihydrofolate (FH2) to tetrahydrofolate (FH4). They are frequently used in cancer chemotherapy. (From AMA, Drug Evaluations Annual, 1994, p2033)

Ring compounds having atoms other than carbon in their nuclei. (Grant & Hackh's Chemical Dictionary, 5th ed)

The complex series of phenomena, occurring between the end of one CELL DIVISION and the end of the next, by which cellular material is duplicated and then divided between two daughter cells. The cell cycle includes INTERPHASE, which includes G0 PHASE; G1 PHASE; S PHASE; and G2 PHASE, and CELL DIVISION PHASE.

A subspecialty of pathology concerned with the molecular basis (e.g., mutations) of various diseases.

Protein kinases that control cell cycle progression in all eukaryotes and require physical association with CYCLINS to achieve full enzymatic activity. Cyclin-dependent kinases are regulated by phosphorylation and dephosphorylation events.

Proteins that control the CELL DIVISION CYCLE. This family of proteins includes a wide variety of classes, including CYCLIN-DEPENDENT KINASES, mitogen-activated kinases, CYCLINS, and PHOSPHOPROTEIN PHOSPHATASES as well as their putative substrates such as chromatin-associated proteins, CYTOSKELETAL PROTEINS, and TRANSCRIPTION FACTORS.

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.

Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.

A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect.

An enzyme of the transferase class that catalyzes the reaction 5,10-methylenetetrahydrofolate and dUMP to dihydrofolate and dTMP in the synthesis of thymidine triphosphate. (From Dorland, 27th ed) EC 2.1.1.45.

The transmission and reproduction of transient images of fixed or moving objects. An electronic system of transmitting such images together with sound over a wire or through space by apparatus that converts light and sound into electrical waves and reconverts them into visible light rays and audible sound. (From Webster, 3rd ed)

Recording of visual and sometimes sound signals on magnetic tape.

A colorless, odorless gas that can be formed by the body and is necessary for the respiration cycle of plants and animals.

A measure of the total greenhouse gas emissions produced by an individual, organization, event, or product. It is measured in units of equivalent kilograms of CARBON DIOXIDE generated in a given time frame.

A nonmetallic element with atomic symbol C, atomic number 6, and atomic weight [12.0096; 12.0116]. It may occur as several different allotropes including DIAMOND; CHARCOAL; and GRAPHITE; and as SOOT from incompletely burned fuel.

Theoretical representations that simulate the behavior or activity of chemical processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment.

Theoretical representations that simulate the behavior or activity of systems, processes, or phenomena. They include the use of mathematical equations, computers, and other electronic equipment.

A rigorously mathematical analysis of energy relationships (heat, work, temperature, and equilibrium). It describes systems whose states are determined by thermal parameters, such as temperature, in addition to mechanical and electromagnetic parameters. (From Hawley's Condensed Chemical Dictionary, 12th ed)

Potency and mechanism of action of E4021, a type 5 phosphodiesterase isozyme-selective inhibitor, on the photoreceptor phosphodiesterase depend on the state of activation of the enzyme. (1/3696)

The ability of inhibitors selective for the type 5 phosphodiesterase isozyme (PDE5) to act on the photoreceptor PDE isozyme (PDE6, the central effector enzyme for visual transduction) is poorly understood. Because PDE5 inhibitors are currently used as therapeutic agents, it is important to assess the potency and mechanism of action of this class of PDE inhibitor on PDE6. We show that E4021 (sodium 1-[6-chloro-4-(3, 4-methylenedioxybenzyl)-aminoquinazolin-2-yl]piperidine-4-ca rboxylate sesquihydrate) inhibits activated PDE6 (KI = 1.7 nM) as potently as PDE5. This makes E4021 the most potent inhibitor of PDE6 discovered to date. The effectiveness of E4021 to inhibit nonactivated PDE6 (with bound inhibitory gamma subunits) is reduced 40-fold compared with the activated enzyme. Furthermore, at intermediate E4021 concentrations and high cGMP concentrations, nonactivated PDE undergoes activation of cGMP hydrolysis rather than inhibition. We demonstrate direct competition of E4021 and the gamma subunits for binding to the catalytic site. Measurements of cGMP binding to noncatalytic regulatory sites on the catalytic subunits of PDE6 rule out an allosteric effect of E4021 by direct binding to these noncatalytic sites. We conclude that E4021 is a competitive inhibitor of cGMP hydrolysis and that the gamma subunit also competes with both E4021 and substrate for catalytic site binding. An understanding of the effects of PDE5-targeted drugs on retinal PDE6 requires a knowledge of the complex interactions among substrate, drug, and inhibitory gamma subunit at the catalytic site of both nonactivated and activated forms of PDE6. (+info)

Interactive effects of inhibitors of poly(ADP-ribose) polymerase and DNA-dependent protein kinase on cellular responses to DNA damage. (2/3696)

DNA-dependent protein kinase (DNA-PK) and poly(ADP-ribose) polymerase (PARP) are activated by DNA strand breaks and participate in DNA repair. We investigated the interactive effects of inhibitors of these enzymes [wortmannin (WM), which inhibits DNA-PK, and 8-hydroxy-2-methylquinazolin-4-one (NU1025), a PARP inhibitor] on cell survival and DNA double-strand break (DSB) and single-strand break (SSB) rejoining in Chinese hamster ovary-K1 cells following exposure to ionizing radiation (IR) or temozolomide. WM (20 microM) or NU1025 (300 microM) potentiated the cytotoxicity of IR with dose enhancement factors at 10% survival (DEF10) values of 4.5 +/- 0.6 and 1.7 +/- 0.2, respectively. When used in combination, a DEF10 of 7.8 +/- 1.5 was obtained. WM or NU1025 potentiated the cytotoxicity of temozolomide, and an additive effect on the DEF10 value was obtained with the combined inhibitors. Using the same inhibitor concentrations, their single and combined effects on DSB and SSB levels following IR were assessed by neutral and alkaline elution. Cells exposed to IR were post-incubated for 30 min to allow repair to occur. WM or NU1025 increased net DSB levels relative to IR alone (DSB levels of 1.29 +/- 0.04 and 1.20 +/- 0.05, respectively, compared with 1.01 +/- 0.03 for IR alone) and the combination had an additive effect. WM had no effect on SSB levels, either alone or in combination with NU1025. SSB levels were increased to 1.27 +/- 0.05 with NU1025 compared with IR alone, 1.02 +/- 0.04. The dose-dependent effects of the inhibitors on DSB levels showed that they were near maximal by 20 microM WM and 300 microM NU1025. DSB repair kinetics were studied. Both inhibitors increased net DSB levels over a 3 h time period; when they were combined, net DSB levels at 3 h were identical to DSB levels immediately post-IR. The combined use of DNA repair inhibitors may have therapeutic potential. (+info)

A phase I study of the lipophilic thymidylate synthase inhibitor Thymitaq (nolatrexed dihydrochloride) given by 10-day oral administration. (3/3696)

2-Amino-3,4-dihydro-6-methyl-4-oxo-5-(4-pyridylthio)-quinazoline dihydrochloride (nolatrexed dihydrochloride, Thymitaq, AG337), a specific inhibitor of thymidylate synthase, was developed using protein structure-based drug design. Intravenously administered nolatrexed is active clinically. As oral bioavailability is high (70-100%), nolatrexed was administered orally, 6 hourly for 10 days, at 3-week intervals, and dose escalated from 80 to 572 mg m(-2) day(-1) in 23 patients. Common toxicity criteria (CTC) grade 3 toxicities included nausea, vomiting, stomatitis and liver function test (LFT) abnormalities. Thrombocytopenia (grade 1 or 2) occurred at doses > or = 318 mg m(-2) day(-1) and neutropenia (grade 2) at 429 and 572 mg m(-2) day(-1). An erythematous maculopapular rash occurred at dosages > or = 318 mg m(-2) day(-1) (7 out of 19 patients). LFT abnormalities occurred in two out of six patients (grade 3 or 4 bilirubin and grade 3 alanine transaminase) at 572 mg m(-2) day(-1). Nolatrexed plasma concentrations 1 h after dosing were 6-16 microg ml(-1), and trough 3-8 microg ml(-1), at 572 mg m(-2) day(-1). Inhibition of thymidylate synthase was demonstrated by elevation of plasma deoxyuridine. Six-hourly oral nolatrexed for 10 days was associated with antiproliferative effects, but nausea and vomiting was dose limiting at 572 mg m(-2) day(-1). Nine patients were treated at 429 mg m(-2) day(-1); three out of nine experienced grade 3 nausea, but 17 out of 22 treatment courses were completed (with the co-administration of prophylactic antiemetics) and this dose level could be considered for phase II testing. (+info)

Inhibition of transforming growth factor alpha (TGF-alpha)-mediated growth effects in ovarian cancer cell lines by a tyrosine kinase inhibitor ZM 252868. (4/3696)

The modulating effects of the epidermal growth factor (EGF) receptor-specific tyrosine kinase inhibitor ZM 252868 on cell growth and signalling have been evaluated in four ovarian carcinoma cell lines PE01, PE04, SKOV-3 and PE01CDDP. Transforming growth factor alpha (TGF-alpha)-stimulated growth was completely inhibited by concentrations > or =0.3 microM in the PE01 and PE04 cell lines and by > or =0.1 microM in SKOV-3 cells. TGF-alpha inhibition of PE01CDDP growth was reversed by concentrations > or =0.1 microM ZM 252868. TGF-alpha-stimulated tyrosine phosphorylation of both the EGF receptor and c-erbB2 receptor in all four cell lines. The inhibitor ZM 252868, at concentrations > or =0.3 microM, completely inhibited TGF-alpha-stimulated tyrosine phosphorylation of the EGF receptor and reduced phosphorylation of the c-erbB2 protein. EGF-activated EGF receptor tyrosine kinase activity was completely inhibited by 3 microM ZM 252868 in PE01, SKOV-3 and PE01CDDP cells. These data indicate that the EGF receptor-targeted TK inhibitor ZM 252868 can inhibit growth of ovarian carcinoma cells in vitro consistent with inhibition of tyrosine phosphorylation at the EGF receptor. (+info)

Keratinocyte collagenase-1 expression requires an epidermal growth factor receptor autocrine mechanism. (5/3696)

In response to cutaneous injury, expression of collagenase-1 is induced in keratinocytes via alpha2beta1 contact with native type I collagen, and enzyme activity is essential for cell migration over this substratum. However, the cellular mechanism(s) mediating integrin signaling remain poorly understood. We demonstrate here that treatment of keratinocytes cultured on type I collagen with epidermal growth factor receptor (EGFR) blocking antibodies or a specific receptor antagonist inhibited cell migration across type I collagen and the matrix-directed stimulation of collagenase-1 production. Additionally, stimulation of collagenase-1 expression by hepatocyte growth factor, transforming growth factor-beta1, and interferon-gamma was blocked by EGFR inhibitors, suggesting a required EGFR autocrine signaling step for enzyme expression. Collagenase-1 mRNA was not detectable in keratinocytes isolated immediately from normal skin, but increased progressively following 2 h of contact with collagen. In contrast, EGFR mRNA was expressed at high steady-state levels in keratinocytes isolated immediately from intact skin but was absent following 2 h cell contact with collagen, suggesting down-regulation following receptor activation. Indeed, tyrosine phosphorylation of the EGFR was evident as early as 10 min following cell contact with collagen. Treatment of keratinocytes cultured on collagen with EGFR antagonist or heparin-binding (HB)-EGF neutralizing antibodies dramatically inhibited the sustained expression (6-24 h) of collagenase-1 mRNA, whereas initial induction by collagen alone (2 h) was unaffected. Finally, expression of collagenase-1 in ex vivo wounded skin and re-epithelialization of partial thickness porcine burn wounds was blocked following treatment with EGFR inhibitors. These results demonstrate that keratinocyte contact with type I collagen is sufficient to induce collagenase-1 expression, whereas sustained enzyme production requires autocrine EGFR activation by HB-EGF as an obligatory intermediate step, thereby maintaining collagenase-1-dependent migration during the re-epithelialization of epidermal wounds. (+info)

A novel class of lipophilic quinazoline-based folic acid analogues: cytotoxic agents with a folate-independent locus. (6/3696)

Three lipophilic quinazoline-based aminomethyl pyridine compounds, which differ only in the position of the nitrogen in their pyridine ring, are described. CB300179 (2-pyridine), CB300189 (4-pyridine) and CB30865 (3-pyridine) all inhibited isolated mammalian TS with IC50 values of 508, 250 and 156 nM respectively. CB30865 was the most potent growth inhibitory agent (IC50 values in the range 1-100 nM for several mouse and human cell types). CB300179 and CB300189 were active in the micromolar range. Against W1L2 cells, CB300179 and CB300189 demonstrated reduced potency in the presence of exogenous thymidine (dThd), and against a W1L2:C1 TS overproducing cell line. In contrast, CB30865 retained activity in these systems. Furthermore, combinations of precursors and end products of folate metabolism, e.g. dThd/hypoxanthine (HX) or leucovorin (LV), did not prevent activity. CB30865 did not interfere with the incorporation of tritiated dThd, uridine or leucine after 4 h. A cell line was raised with acquired resistance to CB30865 (W1L2:R865; > 200-fold), which was not cross-resistant to CB300179 or CB300189. In addition, W1L2:R865 cells were as sensitive as parental cells to agents from all the major chemotherapeutic drug classes. CB300179 and CB300189 induced an S phase accumulation (preventable by co-administration of dThd). No cell cycle redistribution was observed following exposure (4-48 h) to an equitoxic concentration of CB30865. In the NCI anticancer drug-discovery screen, CB30865 displayed a pattern of activity which was not consistent with known anti-tumour agents. These data suggest that CB30865 represents a class of potent potential anti-tumour agents with a novel mechanism of action. (+info)

Activation-dependent clustering of the erbB2 receptor tyrosine kinase detected by scanning near-field optical microscopy. (7/3696)

ErbB2 (HER2, Neu), a member of the epidermal growth factor (EGF) receptor tyrosine kinase family, is often overexpressed in breast cancer and other malignancies. ErbB2 homodimerizes but also presents as a common auxiliary subunit of the EGF and heregulin receptors (erbB1 or EGFR; and erbB3-4, respectively), with which it heteroassociates. ErbB2 is generally regarded as an orphan (ligand-less) receptor with a very potent kinase domain activated either via its associated partners or constitutively as a consequence of discrete mutations. It follows that the extent and regulation of its cell surface interactions are of central importance. We have studied the large-scale association pattern of erbB2 in quiescent and activated cells labeled with fluorescent anti-erbB2 monoclonal antibodies using scanning near-field optical microscopy (SNOM). ErbB2 was found to be concentrated in irregular membrane patches with a mean diameter of approx. 0.5 microm in nonactivated SKBR3 and MDA453 human breast tumor cells. The average number of erbB2 proteins in a single cluster on nonactivated SKBR3 cells was about 10(3). Activation of SKBR3 cells with EGF, heregulin as well as a partially agonistic anti-erbB2 monoclonal antibody led to an increase in the mean cluster diameter to 0.6-0.9 microm, irrespective of the ligand. The EGF-induced increase in the erbB2 cluster size was inhibited by the EGFR-specific tyrosine kinase inhibitor PD153035. The average size of erbB2 clusters on the erbB2-transfected line of CHO cells (CB2) was similar to that of activated SKBR3 cells, a finding correlated with the increased base-line tyrosine phosphorylation of erbB2 in cells expressing only erbB2. We conclude that an increase in cluster size may constitute a general phenomenon in the activation of erbB2. (+info)

Pleiotropic coupling of G protein-coupled receptors to the mitogen-activated protein kinase cascade. Role of focal adhesions and receptor tyrosine kinases. (8/3696)

G protein-coupled receptors (GPCRs) initiate Ras-dependent activation of the Erk 1/2 mitogen-activated protein kinase cascade by stimulating recruitment of Ras guanine nucleotide exchange factors to the plasma membrane. Both integrin-based focal adhesion complexes and receptor tyrosine kinases have been proposed as scaffolds upon which the GPCR-induced Ras activation complex may assemble. Using specific inhibitors of focal adhesion complex assembly and receptor tyrosine kinase activation, we have determined the relative contribution of each to activation of the Erk 1/2 cascade following stimulation of endogenous GPCRs in three different cell types. The tetrapeptide RGDS, which inhibits integrin dimerization, and cytochalasin D, which depolymerizes the actin cytoskeleton, disrupt the assembly of focal adhesions. In PC12 rat pheochromocytoma cells, both agents block lysophosphatidic acid (LPA)- and bradykinin-stimulated Erk 1/2 phosphorylation, suggesting that intact focal adhesion complexes are required for GPCR-induced mitogen-activated protein kinase activation in these cells. In Rat 1 fibroblasts, Erk 1/2 activation via LPA and thrombin receptors is completely insensitive to both agents. Conversely, the epidermal growth factor receptor-specific tyrphostin AG1478 inhibits GPCR-mediated Erk 1/2 activation in Rat 1 cells but has no effect in PC12 cells. In HEK-293 human embryonic kidney cells, LPA and thrombin receptor-mediated Erk 1/2 activation is partially sensitive to both the RGDS peptide and tyrphostin AG1478, suggesting that both focal adhesion and receptor tyrosine kinase scaffolds are employed in these cells. The dependence of GPCR-mediated Erk 1/2 activation on intact focal adhesions correlates with expression of the calcium-regulated focal adhesion kinase, Pyk2. In all three cell types, GPCR-stimulated Erk 1/2 activation is significantly inhibited by the Src kinase inhibitors, herbimycin A and 4-amino-5-(4-methylphenyl)-7-(t-butyl)pyrazolo-D-3,4-pyrimidine (PP1), suggesting that Src family nonreceptor tyrosine kinases represent a point of convergence for signals originating from either scaffold. (+info)

Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic acids: Clonixeril. *Clonixin. *Flunixin; Sulfonanilides: ...

https://en.wikipedia.org/wiki/Selexipag

Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic acids: Clonixeril. *Clonixin. *Flunixin; Sulfonanilides: ...

https://en.wikipedia.org/wiki/Fenamic_acid

Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic acids: Clonixeril. *Clonixin. *Flunixin; Sulfonanilides: ...

https://en.wikipedia.org/wiki/Cysteinyl_leukotriene_receptor_2

... (marketed by King Pharmaceuticals under the brand name Skelaxin) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions. Its exact mechanism of action is not known, but it may be due to general central nervous system depression. It is considered to be a moderately strong muscle relaxant, with relatively low incidence of side effects. Skelaxin is available in an 800 mg scored tablet. Possible side effects include nausea, vomiting, drowsiness and CNS side effects, such as dizziness, headache, and irritability. The metabolism of metaxalone involves the liver cytochrome P450 system. Based on the information in the labeling, patients receiving metaxalone therapy and physicians prescribing metaxalone are directed to take precaution when coadministering it with other medications involving the P450 system.[1][2] Because of potential for side effects, this drug is considered high risk in the elderly. As of 2015[update] the ...

https://en.wikipedia.org/wiki/Metaxalone

Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic acids: Clonixeril. *Clonixin. *Flunixin; Sulfonanilides: ...

https://en.wikipedia.org/wiki/Gamma-Linolenic_acid

While botulinum toxin is generally considered safe in a clinical setting, there can be serious side effects from its use. The use of botulinum toxin A in cerebral palsy children is safe in the upper and lower limb muscles.[5][6] Most commonly, botulinum toxin can be injected into the wrong muscle group or with time spread from the injection site, causing temporary paralysis of unintended muscles. Side effects from cosmetic use generally result from unintended paralysis of facial muscles. These include partial facial paralysis, muscle weakness, and trouble swallowing. Side effects are not limited to direct paralysis however, and can also include headaches, flu-like symptoms, and allergic reactions.[41] Just as cosmetic treatments only last a number of months, paralysis side-effects can have the same durations.[citation needed] At least in some cases, these effects are reported to dissipate in the weeks after treatment.[citation needed] Bruising at the site of injection is not a side effect of the ...

https://en.wikipedia.org/wiki/Botulinum

Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic acids: Clonixeril. *Clonixin. *Flunixin; Sulfonanilides: ...

https://en.wikipedia.org/wiki/Prostaglandin_receptor

... is a centrally acting muscle relaxant. It can be used as an antidote for strychnine poisoning. Mephenesin however presents with the major drawbacks of having a short duration of action and a much greater effect on the spinal cord than the brain, resulting in pronounced respiratory depression at clinical doses and therefore a very low therapeutic index. It is especially dangerous and potentially fatal in combination with alcohol and other depressants.[1] Mephenesin was used by Bernard Ludwig and Frank Berger to synthesize meprobamate, the first tranquilizer to see widespread clinical use. Mephenesin is no longer available in North America but is used in France, Italy and a few other countries.[2] Its use has largely been replaced by the related drug methocarbamol, which is better absorbed.[3] Mephenesin may be an NMDA receptor antagonist.[4] ...

https://en.wikipedia.org/wiki/Mephenesin

Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic acids: Clonixeril. *Clonixin. *Flunixin; Sulfonanilides: ...

https://en.wikipedia.org/wiki/COX_inhibitor

Neuromuscular blocking agents need to fit in a space close to 2 nanometres, which resembles the molecular length of decamethonium.[13] Some molecules of decamethonium congeners may bind only to one receptive site. Flexible molecules have a greater chance of fitting receptive sites. However, the most populated conformation may not be the best-fitted one. Very flexible molecules are, in fact, weak neuromuscular inhibitors with flat dose-response curves. On the other hand, stiff or rigid molecules tend to fit well or not at all. If the lowest-energy conformation fits, the compound has high potency because there is a great concentration of molecules close to the lowest-energy conformation. Molecules can be thin but yet rigid.[14] Decamethonium for example needs relatively high energy to change the N-N distance.[13] In general, molecular rigidity contributes to potency, while size affects whether a muscle relaxant shows a polarizing or a depolarizing effect.[3] Cations must be able to flow through ...

https://en.wikipedia.org/wiki/Neuromuscular-blocking_drug

Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic acids: Clonixeril. *Clonixin. *Flunixin; Sulfonanilides: ...

https://en.wikipedia.org/wiki/Selenium_disulfide

Because of the enhancement of inhibition in the CNS, most spasmolytic agents have the side effects of sedation, drowsiness and may cause dependence with long-term use. Several of these agents also have abuse potential, and their prescription is strictly controlled.[22][23][24] The benzodiazepines, such as diazepam, interact with the GABAA receptor in the central nervous system. While it can be used in patients with muscle spasm of almost any origin, it produces sedation in most individuals at the doses required to reduce muscle tone.[5] Baclofen is considered to be at least as effective as diazepam in reducing spasticity, and causes much less sedation. It acts as a GABA agonist at GABAB receptors in the brain and spinal cord, resulting in hyperpolarization of neurons expressing this receptor, most likely due to increased potassium ion conductance. Baclofen also inhibits neural function presynaptically, by reducing calcium ion influx, and thereby reducing the release of excitatory ...

https://en.wikipedia.org/wiki/Skeletal_muscle_relaxant

... ( anticholinergic agent) is a group of substances that blocks the action of the neurotransmitter acetylcholine (ACh) at synapses in the central and the peripheral nervous system, and, in broad terms, neuromuscular junction.[1][2] These agents inhibit parasympathetic nerve impulses by selectively blocking the binding of the neurotransmitter acetylcholine to its receptor in nerve cells. The nerve fibers of the parasympathetic system are responsible for the involuntary movement of smooth muscles present in the gastrointestinal tract, urinary tract, lungs, and many other parts of the body;[3] cholinergic process otherwise by enhancing ACh function.[3] In broad terms, anticholinergics are divided into two categories in accordance with their specific targets in the central, peripheral nervous system and neuromuscular junction:[3] antimuscarinic agents, and antinicotinic agents (ganglionic blockers, neuromuscular blockers).[4] In strict terms, anticholinergic only comprises ...

https://en.wikipedia.org/wiki/Anticholinergics

The usual dose of 350 mg is unlikely to engender prominent side effects other than somnolence, and mild to significant euphoria or dysphoria, but the euphoria is generally short-lived due to the fast metabolism of carisoprodol into meprobamate and other metabolites; the euphoria derived is, according to new research, most likely due to carisoprodol's inherent, potent anxiolytic effects that are far stronger than those produced by its primary metabolite, meprobamate, which is often misblamed for the drug-seeking associated with carisoprodol, as carisoprodol itself is responsible for the significantly more intense CNS effects than meprobamate alone. Carisoprodol has a unique mechanism of action, qualitatively different from that of meprobamate (Miltown). The medication is well-tolerated and without adverse effects in the majority of patients for whom it is indicated. In some patients, however, and/or early in therapy, carisoprodol can have the full spectrum of sedative side effects and can impair ...

https://en.wikipedia.org/wiki/Carisoprodol

InChI=1S/C40H48N2O6.2ClH/c1-41(2)17-15-27-22-34(44-6)36-24-30(27)31(41)19-25-9-12-29(13-10-25)47-40-38-28(23-37(45-7)39(40)46-8)16-18-42(3,4)32(38)20-26-11-14-33(43-5)35(21-26)48-36;;/h9-14,21-24,31-32H,15-20H2,1-8H3;2*1H/q+2;;/p-2/t31-,32+;;/m0../ ...

https://en.wikipedia.org/wiki/Dimethyltubocurarine

It was designed to be a weaker antagonist at the neuromuscular junction than pancuronium; hence its monoquaternary structure and its having an allyl group and a pyrrolidine group attached to the D ring quaternary nitrogen atom. Rocuronium has a rapid onset and intermediate duration of action.[2] There is considered to be a risk of allergic reaction to the drug in some patients (particularly those with asthma), but a similar incidence of allergic reactions has been observed by using other members of the same drug class (non-depolarizing neuromuscular blocking drugs).[3] The γ-cyclodextrin derivative sugammadex (trade name Bridion) has been recently introduced as a novel agent to reverse the action of rocuronium.[4] Sugammadex has been in use since 2009 in many European countries; however, it was turned down for approval twice by the US FDA due to concerns over allergic reactions and bleeding,[5] but finally approved the medication for use during surgical procedures in the United States on ...

https://en.wikipedia.org/wiki/Rocuronium_bromide

Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic acids: Clonixeril. *Clonixin. *Flunixin; Sulfonanilides: ...

https://en.wikipedia.org/wiki/Cyclooxygenase-2

InChI=1S/C27H33NO10S/c1-12(30)28-16-7-5-13-9-18(37-27-24(34)23(33)22(32)19(11-29)38-27)25(35-2)26(36-3)21(13)14-6-8-20(39-4)17(31)10-15(14)16/h6,8-10,16,19,22-24,27,29,32-34H,5,7,11H2,1-4H3,(H,28,30)/t16-,19+,22+,23-,24+,27+/m0/s1 ...

https://en.wikipedia.org/wiki/Thiocolchicoside

Sternbach LH, Fryer RI, Keller O, Metlesics W, Sach G, Steiger N (May 1963). "Quinazolines and 1,4-Benzodiazepines. X. Nitro- ...

https://en.wikipedia.org/wiki/Nitrazepam

... (peganine) is a quinazoline alkaloid. It is found in Justicia adhatoda, after which it is named. It is additionally ... Nepali, Kunal; Sharma, Sahil; Ojha, Ritu; Dhar, Kanaya Lal (2012). "Vasicine and structurally related quinazolines". Medicinal ...

https://en.wikipedia.org/wiki/Vasicine

... is a heterocyclic chemical compound, a quinazoline with a carbonyl group in the C4N2 ring. Two isomers are ... 2016), "Quinazolinone and quinazoline derivatives: recent structures with potent antimicrobial and cytotoxic activities", Res ... 2-Quinazolinone 4-Quinazolinone Common routes to quinazolines involve condensation of amides to anilines with ortho nitrile, ... "Synthesis of quinazolinones and quinazolines". Tetrahedron. 61 (43): 10153-10202. doi:10.1016/j.tet.2005.07.010.. ...

https://en.wikipedia.org/wiki/Quinazolinone

Archer GA, Sternbach LH (1964). "Quinazolines and 1,4-Benzodiazepines. XVI. Synthesis and Transformations of 5-Phenyl-1,4- ...

https://en.wikipedia.org/wiki/Sulazepam

Walser, A, Zenchoff G (1977). "Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative ...

https://en.wikipedia.org/wiki/Alprazolam

11-Chloro-5-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-2,3-dihydrodiimidazo[1,2-c:1',5'-a]quinazoline ...

https://en.wikipedia.org/wiki/U-90042

8-quinoline > 8-quinazoline > 8-isoquinoline ≥ cinnoline > phthalazine > quinoxaline > 5-quinoline e.g. AMG-517 (fig. 8b), ... quinazoline, phthalazine, quinoxaline, and cinnoline moieties". Journal of Medicinal Chemistry. 48 (3): 744-52. doi:10.1021/ ...

https://en.wikipedia.org/wiki/Discovery_and_development_of_TRPV1_antagonists

Chemical Encyclopedia: Quinazoline alkaloids. xumuk.ru Aniszewski, p. 106 Aniszewski, p. 105 Richard B. Herbert; Herbert, ...

https://en.wikipedia.org/wiki/Alkaloid

... is a quinazoline alkaloid. It shows bronchodilatory activity in vitro but bronchoconstrictory activity in vivo. ...

https://en.wikipedia.org/wiki/Vasicinone

... is a quinazoline derivative. It is a dihydrofolate reductase inhibitor. It has been used with leucovorin in ...

https://en.wikipedia.org/wiki/Trimetrexate

ISBN 978-0122830600 1997: Des Brown & Damon Ridley, Quinazolines. Supplement 1: The Chemistry of Heterocyclic Compounds (Brown ...

https://en.wikipedia.org/wiki/Ollé_Prize

Vögtle, Markus M.; Marzinzik, Andreas L. (July 2004). "Synthetic Approaches Towards Quinazolines, Quinazolinones and ...

https://en.wikipedia.org/wiki/Hypnotic

The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...

https://webbook.nist.gov/cgi/inchi/InChI%3D1S/C8H6N2/c1-2-4-8-7

Quinazolinone Niementowski quinazoline synthesis Armarego, W. L. F. (1963). "Quinazolines". Advances in Heterocyclic Chemistry ... Over 200 biologically active quinazoline and quinoline alkaloids are identified. The synthesis of quinazoline was first ... Quinazoline is an organic compound with the formula C8H6N2. It is an aromatic heterocycle with a bicyclic structure consisting ... Quinazoline protonates (and methylates) at N3. Protonation induces hydration. Many mildly acidic substrates add across the C=N3 ...

https://en.wikipedia.org/wiki/Quinazoline

Quinazoline derivatives have found applications as anti-malarial agents and in cancer treatment. The presence of a halogen ... Quinazoline is composed of fused benzene and pyrimidine rings. ... quinazoline AldrichCPR C8H3ClFN3O2 * pricing ... Quinazoline is composed of fused benzene and pyrimidine rings. Quinazoline derivatives have found applications as anti-malarial ... quinazoline AldrichCPR C8H4FN3O3 * pricing ...

https://www.sigmaaldrich.com/chemistry/chemistry-products.html?TablePage=16271308

Quinazoline alkaloids are natural products from the group of alkaloids, which are chemically derived from quinazoline. Some ... quinazolines and indoloquinazolines. Vasicine Evodiamine Rutaecarpine Febrifugine Quinazoline alkaloids can be found mainly in ... About 70 alkaloids with a quinazoline structure are known, which are mostly further classified as simple quinazolinones, ... quinazoline alkaloids show bronchodilatory effects and stimulate respiration. An abortive effect was also found for vasicine in ...

https://en.wikipedia.org/wiki/Quinazoline_alkaloids

Quinazoline, Alkylquinazolines, and Arylquinazolines.. Halogenoquinazolines.. Oxyquinazolines.. Thioquinazolines.. Nitro, Amino ... Due to the vast increase in the number and types of individual quinazolines described in recent literature, the author has ... replaced the myriad classified tables of known quinazolines with a single alphabetical table of simple known quinazolines. To ... and Related Quinazolines.. Quinazolinecarboxylic Acids and Related Derivatives.. Appendix.. References.. Index. ...

https://www.wiley.com/en-us/Quinazolines%2C+Supplement+1%2C+Volume+55-p-9780471145653

... ...

https://www.ncbi.nlm.nih.gov/Structure/pdb/2W0V

W. L. F. Armarego, A Text Book of Quinazolines, 1963. *R. Rajput and A. P. Mishra, "A review on biological activity of ... I. P. Jung, H. L. So, S. C. Chan, and S. K. Kwan, "Study on the selective reduction of 1H-quinazoline-2,4-diones," Bulletin of ... B. Pati and S. Banerjee, "Quinazolines: an illustrated review," Journal of Advanced Pharmacy. Education & Research, vol. 3, no ... H.-Q. Li, D.-D. Li, X. Lu, Y.-Y. Xu, and H.-L. Zhu, "Design and synthesis of 4,6-substituted-(diaphenylamino)quinazolines as ...

https://www.hindawi.com/journals/ijmc/2014/395637/ref/

Biotransformation of quinazoline and phthalazine by Aspergillus niger.. [John B Sutherland, Thomas M Heinze, Laura K ... Quinazoline was oxidized to 4-quinazolinone and 2,4-quinazolinedione, and phthalazine was oxidized to 1-phthalazinone. ... Cultures of Aspergillus niger NRRL-599 in fluid Sabouraud medium were grown with quinazoline and phthalazine for 7 days. ...

https://www.sigmaaldrich.com/catalog/papers/21169055

The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.. Newton R1, ... The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity ... The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity ... The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity ...

https://www.ncbi.nlm.nih.gov/pubmed/26874741

... quinazolines. The latter were, in turn, subjected to sequential (Sonogashira and Suzuki-Miyaura) and one-pot two-step ( ... quinazolines. The imidazoquinazolines were screened for in vitro cytotoxicity against human breast adenocarcinoma (MCF-7) cells ... quinazolines; cytotoxicity dihalogenated 2H-imidazo[1,2-c]quinazolines; cross-coupling; imidazo[1,2-c]quinazolines; ... Novel Polycarbo-Substituted Imidazo[1,2-c]quinazolines: Synthesis and Cytotoxicity Study. Tebogo Ankie Khoza 1. ...

http://www.mdpi.com/1420-3049/20/12/19863

2WZ6: Structural Discovery of Small Molecule Binding Sites in Cu-Zn Human Superoxide Dismutase Familial Amyotrophic Lateral Sclerosis Mutants Provides Insights for Lead Optimization.

http://www.rcsb.org/pdb/explore/structureCluster.do?structureId=2WZ6

A compound of formula (I) wherein A, X, Y, Z, R.sub.1 and R.sub.24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, I.sub.Kur-associated disorders, and other disorders mediated by ion channel function. ##STR00001##

http://www.patentgenius.com/patent/8575184.html

... quinazolines. The latter were, in turn, subjected to sequential (Sonogashira and Suzuki-Miyaura) and one-pot two-step ( ... quinazolines. The imidazoquinazolines were screened for in vitro cytotoxicity against human breast adenocarcinoma (MCF-7) cells ... quinazolines; cytotoxicity dihalogenated 2H-imidazo[1,2-c]quinazolines; cross-coupling; imidazo[1,2-c]quinazolines; ... In Vitro Cytotoxicity of Imidazo[1,2-c]quinazolines 3-6. Twenty two (22) of the imidazo[1,2-c]quinazolines were evaluated for ...

https://www.mdpi.com/1420-3049/20/12/19863/htm

For example, reaction of 2-chloro-4-(4-methylpiperazin-1-yl)quinazoline with N-methyl-4-chlorobenzenesulfonamide gave II in 10 ... quinazoline piperazinyl benzenesulfonamide prepn 5HT6 modulator, Alzheimer schizophrenia obesity Parkinson disease treatment ...

http://uu.diva-portal.org/smash/record.jsf?pid=diva2:888187

Substituted quinazolines of the formula (1): ##STR1## wherein: R 1 to R 4 are independently H, halo, (C 1 -C 4 ) alkyl, ... C07D239/72-Quinazolines; Hydrogenated quinazolines * C07D239/74-Quinazolines; Hydrogenated quinazolines with only hydrogen ... C07D239/72-Quinazolines; Hydrogenated quinazolines * C07D239/86-Quinazolines; Hydrogenated quinazolines with hetero atoms ... C07D239/72-Quinazolines; Hydrogenated quinazolines * C07D239/86-Quinazolines; Hydrogenated quinazolines with hetero atoms ...

https://patents.google.com/patent/US5411963A/en

A quinazoline compound represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## (wherein ... It relates to a quinazoline compound useful as a medicine exhibiting an inhibitory action on calmodulin-dependent cGMP-PDE. ... C07D239/72-Quinazolines; Hydrogenated quinazolines * C07D239/86-Quinazolines; Hydrogenated quinazolines with hetero atoms ... Process for preparing quinazolines JPS53103484A (en) * 1977-02-21. 1978-09-08. Takeda Chem Ind Ltd. Quinazoline derivatives, ...

https://patents.google.com/patent/US5614627A/en

Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C.. Zeng, M., Lu, J., Li, L., Feru, F., Quan, C., Gero, T.W., ... KRAS G12C in bound to quinazoline based switch II pocket (SWIIP) binder. *DOI: 10.2210/pdb5V9L/pdb ... Notably we find that adding an amide substituent to the quinazoline scaffold allows additional interactions with KRAS G12C, and ... Optimized lead compounds in the quinazoline series selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at ...

https://www.rcsb.org/structure/5V9L

These treatment failures proved to be due to emergence of parasites resistant to the quinazolines. ... each of these quinazolines effected cure of infections with the Oak Knoll strain at a remarkably small daily dose. However, ... suggesting that the activities of these quinazolines, like those of 6-amino-substituted derivatives, were compromised by ... Studies on the 2,4-Diamino-6-Substituted Quinazolines II. Activities of Selected Derivatives against Infections with Various ...

http://www.ajtmh.org/content/journals/10.4269/ajtmh.1979.28.793

Base-promoted Lewis acid catalyzed synthesis of quinazoline derivatives F. Hu, X. Cui, G. Lu and G. Huang, Org. Biomol. Chem., ...

https://pubs.rsc.org/en/content/articlelanding/2020/ob/d0ob00225a/unauth

For the uses and biological importance of benzothia-zole and quinazoline derivatives, see: Schwartz et al. (1992. ); Wolfe et ... In the title compound, C14H10N2O2S, the benzothia-zole and quinazoline ring systems are essentially planar with maximum ... The quinazoline ring system is also essentially planar with the maximum deviation of -0.1588 (15)Å for the N1 atom. The ... For the uses and biological importance of benzothiazole and quinazoline derivatives, see: Schwartz et al. (1992); Wolfe et al. ...

http://journals.iucr.org/e/issues/2012/11/00/rk2382/index.html

Various quinazoline inhibitors targeting ErbB1 or ErbB2 - 4 have been developed as anti-cancer agents and might be useful for ... Antipsychotic Potential of Quinazoline ErbB1 Inhibitors in a Schizophrenia Model Established With Neonatal Hippocampal ... These results indicate an antipsychotic potential of quinazoline ErbB1 inhibitors. ErbB receptor tyrosine kinases may be novel ...

https://www.jstage.jst.go.jp/article/jphs/114/3/114_10099FP/_article

Design and synthesis of quinazoline derivatives as potential anticancer agents. Ming-Hsieh Chuang, Meng-Ling Chen, Ji-Wang ... Design and synthesis of quinazoline derivatives as potential anticancer agents. Ming-Hsieh Chuang, Meng-Ling Chen, Ji-Wang ... Design and synthesis of quinazoline derivatives as potential anticancer agents. Ming-Hsieh Chuang, Meng-Ling Chen, Ji-Wang ... Design and synthesis of quinazoline derivatives as potential anticancer agents Message Subject (Your Name) has forwarded a page ...

http://mct.aacrjournals.org/content/6/11_Supplement/A2

This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I ##STR00001## wherein Ar, R.sup.1 ... C. for 1.5 h. After cooling to RT the solvent is evaporated giving rise to crude 4,5-dichloro-7-iodo-quinazoline. To a mixture ... STR00065## 4,5,7-substituted quinazolines of the general formula 3-4, wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as ... Sulfoximine substituted quinazolines for pharmaceutical compositions Abstract. This invention relates to novel sulfoximine ...

http://patents.com/us-9708274.html

JoVE publishes peer-reviewed scientific video protocols to accelerate biological, medical, chemical and physical research. Watch our scientific video articles.

https://www.jove.com/v/53662?language=Japanese

... a novel series of quinazoline derivatives is developed for cancer therapy. All the synthesised analogues were evaluated against ... Novel amide analogues of quinazoline carboxylate display selective antiproliferative activity and potent EGFR inhibition. *. ... AbstractIn the present study, a novel series of quinazoline derivatives is developed for cancer therapy. All the synthesised ... The current investigation could be extremely helpful for the development of newer therapeutically useful quinazoline based ...

https://medworm.com/825964988/novel-amide-analogues-of-quinazoline-carboxylate-display-selective-antiproliferative-activity-and-po/

Buy Quinazoline (CAS 253-82-7), a specialty product for proteomics research, from Santa Cruz. Molecular Formula: C8H6N2, ... Quinazoline (CAS 253-82-7) *bvseo_sdk, java_sdk, bvseo-3.2.0 ...

https://www.scbt.com/p/quinazoline-253-82-7/

Quinazoline is a heterocycle and is, for example, a subunit of many anti-cancer drugs. Up to now, the synthesis of quinazoline ... Like Dominoes: Metal-Free Synthesis of Quinazolines News May 03, 2017 , Original Story from the Friederich-Alexander ... In addition, the novel quinazolines have shown that they are highly effective against herpes viruses, and in contrast to many ... This novel one-pot domino process creates a completely new type of quinazolines, which have intrinsic fluorescence properties. ...

https://www.technologynetworks.com/drug-discovery/news/quinazolines-made-using-metal-free-domino-process-288312

Of 11 quinazolines tested in the secondary assay, 8 quinazolines showed activity superior to doxycycline (Fig. 4F). Members of ... 7 Quinazoline CBR715 demonstrates antiwolbachial efficacy in mouse models of B. malayi and O. ochengi filarial infection.. (A) ... 6 Quinazolines demonstrate antiwolbachial efficacy in mouse model of L. sigmodontis filarial infection.. (A and B) Advanced ... Advanced quinazoline lead eliminates Wolbachia in B. malayi and Onchocerca adult worms in vivo. Because of the demonstrated ...

https://stm.sciencemag.org/content/11/491/eaav3523

... quinazolines of the formula: ##STR1## wherein R is (1-pyrrolidinyl)propyl; 3-[bis-(2-hydroxyethyl)amino]propyl; 2,3- ... A mixture of 45 g. (0.145 mole) of 4-chloro-2-(3,4-dichlorophenyl)quinazoline and 44 g. (0.3 mole) of 1-amino-3-diethylamino-2- ... A mixture of 46.5 g. (0.15 mole) of 4-chloro-2-(3,4-dichlorophenyl)quinazoline in 500 ml of dimethylformamide and 29 g (0.31 ... 2-(3,4-Dichlorophenyl)-4-(substituted amino)-quinazolines Abstract. A series of 2-(3,4-dichlorophenyl)-4-(substituted amino) ...

http://patents.com/us-3997538.html

Quinazoline-4(3H) is one of the most frequently encountered heterocycles in medicinal chemistry, which contains a pyrimidine ... Hence in view of the analytical and biological importance of quinazoline-4(3H) and as a part of our continued work on the ... Previously it was reported that quinazoline-4-(3H)-one derivatives have interesting antimicrobial activity against different ... N-Donor Environment of Quinazoline-4(3H)-one Schiff Base and Their Biological Studies,. The Scientific World Journal,. vol. ...

https://www.hindawi.com/journals/tswj/2014/817365/

Quinazoline derivatives have found applications as anti-malarial agents and in cancer treatment. (sigmaaldrich.com)
Though the parent quinazoline molecule is rarely mentioned by itself in technical literature, substituted derivatives have been synthesized for medicinal purposes such as antimalarial and anticancer agents. (wikipedia.org)
7. 2- and 4-halo derivatives of quinazoline undergo displacement by nucleophiles, such as piperidine. (wikipedia.org)
A. K. Mahato, B. Srivastava, and S. Nithya, "Chemistry structure activity relationship and biological activity of quinazoline-4(3 H )-one derivatives," Inventi Rapid: MedChem , vol. 2, no. 1, 2011. (hindawi.com)
Quinazoline derivatives and pharmacological activities: a review," International Journal of Medicinal Chemistry & Analysis , vol. 3, no. 1, pp. 10-21, 2013. (hindawi.com)
Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors," Bioorganic and Medicinal Chemistry Letters , vol. 19, no. 8, pp. 2277-2281, 2009. (hindawi.com)
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation, part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives," Bioorganic and Medicinal Chemistry Letters , vol. 13, no. 18, pp. 3001-3004, 2003. (hindawi.com)
However, doses required for cure of infections with the Camp-CH/Q strain were from 4-48 times those required for cure of infections with the Oak Knoll strain, suggesting that the activities of these quinazolines, like those of 6-amino-substituted derivatives, were compromised by pyrimethamine resistance. (ajtmh.org)
Quinazoline derivatives have been reported to possess various biological activities. (aacrjournals.org)
Thus, the methoxy group was introduced onto quinazoline derivatives at the 6- and 7-position to expect better inhibitory activity. (aacrjournals.org)
AbstractIn the present study, a novel series of quinazoline derivatives is developed for cancer therapy. (medworm.com)
Previously it was reported that quinazoline-4-(3H)-one derivatives have interesting antimicrobial activity against different species of gram-positive, gram-negative, and pathogenic fungi [ 4 ]. (hindawi.com)
In addition, many substituted quinazoline derivatives have recently earned great interest in chemotherapy as antitumor drugs [ 8 ]. (hindawi.com)
The book entitled "Triazolo Quinazolines: Synthesis and Biological Prediction Study" includes a comprehensive review of MW reactions and the Synthesis, Characterization and Biological Prediction Study of Triazolo Quinazoline Derivatives. (morebooks.de)
In the present study, we evaluated cytotoxic effects of various styrylquinazoline derivatives and found that (E)-8-acetoxy-2-[2-(3,4-diacetoxyphenyl)ethenyl]-quinazoline (8-ADEQ) most potently inhibited the proliferation of the human cervical carcinoma HeLa cells. (spandidos-publications.com)
Many quinazoline derivatives were reported to have potent cytotoxic activity. (eurekaselect.com)
Method: Novel series of 4-substituted 6,8-dibromo-2-(4-chlorophenyl)-quinazoline derivatives have been designed and synthesized. (eurekaselect.com)
Method: Synthesis, 2D-QSAR and drug-like physicochemical properties of a set of quinazolinone and quinazoline derivatives were studied as trypanocidal agents. (eurekaselect.com)
Conclusion: The antiprotozoal activity of these quinazolinone and quinazoline derivatives represents an interesting starting point for a medicinal chemistry program aiming at the development of novel chemotherapies for Chagas disease. (eurekaselect.com)
Gholami, Milad 2013-11-30 00:00:00 A simple and facile synthesis of highly functionalized quinazoline derivatives has been successfully developed by treatment of aldehydes, ammonium acetate, and 2-aminoaryl ketones or isatoic anhydride under reflux conditions in the presence of a pentafluorophenylammonium triflate (PFPAT) organocatalyst. (deepdyve.com)
We developed a straightforward method for making isatoic anhydride-8-amide from isatin-7-carboxylic acid as a tool to easily produce a range of quinazoline and substituted aniline derivatives using adaptable pH-sensitive cyclization chemistry. (elsevier.com)
The approaches are inexpensive, simple, fast, efficient at room temperature and scalable, enabling the synthesis of both established and new quinazolines and also highly substituted anilines including cyano derivatives. (elsevier.com)
Materials and Methods: A dataset of 47 analogues of pyrazolo quinazolines were selected with their inhibitory activity on CDK2/Cyclin A. The derivatives were divided into training and test sets. (elsevier.com)
The present invention relates to quinazoline derivatives, which are useful as medicaments, particularly antipruritic agents, or salts thereof and pharmaceutical compositions containing any of them as active ingredients. (justia.com)
The synthesis of a series of push-pull arylvinyl (styryl), aryl, and arylethynyl quinazoline derivatives by means of different straightforward protocols is reported. (archives-ouvertes.fr)
Electrotopological state indices for atomtype (ETSIAT)were employed to establish a quantitative structure- activity relationship (QSAR) model of antitumor activity for 17 indolo[1,2-b]quinazoline derivatives. (pku.edu.cn)
N=, -NH-, =O, and >N- were closely correlated with the antitumor activities of indol[1,2-b]quinazoline derivatives. (pku.edu.cn)
Prediction of Antitumor Activities of Indolo[1,2-b]Quinazoline Derivatives Using Electrotopological State Indices for AtomTypes[J].Acta Phys. (pku.edu.cn)

Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2," Bioorganic and Medicinal Chemistry , vol. 15, no. 11, pp. 3635-3648, 2007. (hindawi.com)
Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor," Bioorganic and Medicinal Chemistry Letters , vol. 14, no. 19, pp. 4867-4872, 2004. (hindawi.com)
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: Selective inhibitors of Aurora B kinase with potent anti-tumor activity," Bioorganic and Medicinal Chemistry Letters , vol. 18, no. 6, pp. 1904-1909, 2008. (hindawi.com)
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. (nih.gov)
Notably we find that adding an amide substituent to the quinazoline scaffold allows additional interactions with KRAS G12C, and remarkably increases the labeling efficiency, potency, and selectivity of KRAS G12C inhibitors. (rcsb.org)
Various quinazoline inhibitors targeting ErbB1 or ErbB2 - 4 have been developed as anti-cancer agents and might be useful for antipsychotic treatment. (go.jp)
These results indicate an antipsychotic potential of quinazoline ErbB1 inhibitors. (go.jp)
Aims: Our aim in this work is the discovery of potent epidermal growth factor receptor (EGFR) inhibitors with anti-breast cancer activity containing 4-substituted quinazoline pharmacophore. (eurekaselect.com)
Marwa F. Ahmed* and Naja Magdy, "Design and Synthesis of 4-substituted Quinazolines as Potent EGFR Inhibitors with Anti-breast Cancer Activity", Anti-Cancer Agents in Medicinal Chemistry (2017) 17: 832. (eurekaselect.com)
CB30865 (p-[N-(7-bromo-3,4-dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl+ ++)-N-(prop-2-ynyl)amino]-N-(3-pyridylmethyl)benzamide) is a quinazoline-based pyridine-containing compound that emerged from a programme aimed at the development of thymidylate synthase (TS) inhibitors as anticancer agents. (semanticscholar.org)
Our study aims on learning the application of five important binary fingerprinting techniques based on the quantum mechanics involving 2D QSAR studies for designing novel pyrazolo quinazolines as selective inhibitors of CDK2/CyclinA. (elsevier.com)
Quinazoline scaffold has been successfully utilized for development of various inhibitors of tubulin, epidermal growth factor receptor (EGFR), polo like kinases (PLKs), Hedgehog-Gli signaling pathway and protein kinase B (PKB) /Akt pathway. (elsevier.com)
Compounds based on quinazolines have shown efficacies in μM to nM range in various cancer cell lines and thus could be useful scaffolds for development of both apoptosis inducers as well as inhibitors. (elsevier.com)
This compilation is based on various patents published till 2015 and divides the quinazolines in two main categories: Quinazolines as apoptosis inducers and as apoptosis inhibitors. (elsevier.com)

Over 200 biologically active quinazoline and quinoline alkaloids are identified. (wikipedia.org)
Biologically active quinoline and quinazoline alkaloids part I." Medicinal Research Reviews. (wikipedia.org)
Quinazoline alkaloids are natural products from the group of alkaloids, which are chemically derived from quinazoline. (wikipedia.org)
Some quinazoline alkaloids show bronchodilatory effects and stimulate respiration. (wikipedia.org)
About 70 alkaloids with a quinazoline structure are known, which are mostly further classified as simple quinazolinones, pyrroloquinazolines, pyrido[2,1-b]quinazolines and indoloquinazolines. (wikipedia.org)
Vasicine Evodiamine Rutaecarpine Febrifugine Quinazoline alkaloids can be found mainly in plants, such as acanthaceae (Adhatoda vasica), rutaceae, saxifragaceae (Dichroa febrifuga) and in linaria species (Scrophulariaceae) and peganum harmala (Fam. (wikipedia.org)
The quinazoline moiety is a building block for about 150 naturally occurring alkaloids and drugs. (morebooks.de)
A series of quinazoline alkaloids fused with 1,4-benzodiazepinone are isolated from different fungal species or their cultures. (aspeneducationgroup.com)

Also known as 1,3-diazanaphthalene, quinazoline received its name from being an aza derivative of quinoline. (wikipedia.org)
The synthesis of quinazoline was first reported in 1895 by August Bischler and Lang through the decarboxylation of the 2-carboxy derivative (quinazoline-2-carboxylic acid). (wikipedia.org)
Anti-tumor effects of B-2, a novel 2,3-disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazoline derivative, on the human lung adenocarcinoma A549 cell line in vitro and in vivo," Chemico-Biological Interactions , vol. 189, no. 1-2, pp. 90-99, 2011. (hindawi.com)
The quinazoline derivative PVHD121 has anti-cell proliferative activity and inhibits tubulin polymerization by binding to the colchicine site of tubulin. (aspetjournals.org)
We here report a study on the mechanism of action of PVHD121, a quinazoline derivative binding to the colchicine site of tubulin. (aspetjournals.org)
Prevention of hippocampus neuronal damage in ischemic gerbils by a novel lipid peroxidation inhibitor (quinazoline derivative). (aspetjournals.org)
We investigated the effect of a novel quinazoline derivative (KB-5666), a lipid peroxidation inhibitor, on ischemic neuronal damage using Mongolian gerbils. (aspetjournals.org)
The present inventors have found that a quinazoline derivative has a nociceptin antagonism and is useful as an analgesic (see Patent Document 1). (justia.com)
Patent Document 2 describes, as a compound having a carbonylamino group at the 2-position of the quinazoline skeleton, a quinazoline derivative that has a neuropeptide Y (NPY) receptor subtype Y5 inhibitory effect and is useful for pain relief and memory disorder. (justia.com)
Patent Document 3 describes a quinazoline derivative, which is useful for bone diseases. (justia.com)
Patent Document 4 describes a quinazoline derivative, which has a LTB4 (leucotriene B4) antagonism and is useful as an anti-inflammatory. (justia.com)

The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C 3 -C 7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C 3 -C 7 cycloalkyl as substituent of a carboxamide at 3 position of the molecula framework. (patentsencyclopedia.com)
The present invention relates to fungicidal mixtures, comprising at least one quinazoline compound I and one compound II as defined in the description, and to compositions comprising these mixtures. (patentsencyclopedia.com)
The present invention relates to the use of quinazolines of formula (I), wherein the groups Ra to Rd have the meanings given in the claims and specification, in cancer therapy. (justia.com)

The two main synthetic approaches towards imidazo[1,2- c ]quinazolines involve either annulation of quinazoline moiety onto an imidazole framework or a two-step assembly of the imidazole ring onto a quinazoline framework. (mdpi.com)

The work has been a continuation of our work from the series of seven books namely Pyrimidines, Quinazolines, Pyrimidines fused with heterocyclic rings, Novel Pyrazoles part I and Novel Pyrazoles part II, Triazolo Pyrimidines and Thiazolo Pyrimidines. (morebooks.de)
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The peculiarities and differences of 1H- and 13C-NMR spectral patterns of 5-R-2-aryl-5,6-dihydro-[1,2,4]triazolo[1,5-c]quinazolines and their aromatic analogues have been described. (edu.ua)

Imidazo[1,2- c ]quinazoline-based compounds continue to attract attention in synthesis because of their application in pharmaceuticals and materials [ 1 ]. (mdpi.com)
We demonstrate that covalent quinazoline-based switch II pocket (SIIP) compounds effectively suppress GTP loading of KRAS G12C, MAPK phosphorylation, and the growth of cancer cells harboring G12C. (rcsb.org)
Optimized lead compounds in the quinazoline series selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations. (rcsb.org)
Up to now, the synthesis of quinazoline heterocycles was very costly and required many individual steps starting with expensive compounds and reagents. (technologynetworks.com)
In addition, the novel quinazolines have shown that they are highly effective against herpes viruses, and in contrast to many other bioactive compounds, do not damage healthy cells. (technologynetworks.com)
Their synthetic utility was demonstrated by condensation reactions with carbonyl compounds or amines to provide SF 5 -containing quinolines and quinazolines, respectively. (beilstein-journals.org)
The promising anticancer profile of some of the quinazoline based compounds clearly highlights the clinical potential of this heterocycle. (elsevier.com)

Quinazoline ring systems have a prominent feature in medicinal chemistry and possess biological activities such as antimalarial, anticonvulsant, antibacterial, antidiabetic, and anticancer. (morebooks.de)
This review will act as a tool for the researchers working on exploring the anticancer potential of quinazoline as a privileged heterocyclic. (elsevier.com)

One-pot reductive cyclization to antitumor quinazoline precursorsOn resonance interactions in methyl 4-X-benzoates and the effect of 2,6-dimethyl substitution. (easechem.com)

Quinazoline is composed of fused benzene and pyrimidine rings. (sigmaaldrich.com)
This paper presents a first quantitative kinetic model for supercritical water oxidation (SCWO) of quinazoline that describes the formation and interconversion of intermediates and final products at 673-873 K. The set of 11 reaction pathways for phenol, pyrimidine, naphthalene, NH3, etc, involved in the simplified reaction network proved sufficient for fitting the experimental results satisfactorily. (usda.gov)
The pyrimidine yielding from quinazoline is the dominant ring-opening pathway and provides a significant contribution to CO2 formation. (usda.gov)

Facile access to potent antiviral quinazoline heterocycles with fluorescence properties via merging metal-free domino reactions. (technologynetworks.com)

They have developed a novel synthetic route towards antiviral quinazoline heterocycles that have not been described previously in professional literature. (technologynetworks.com)

Cell cycle effects of CB30865, a lipophilic quinazoline-based analogue of the antifolate thymidylate synthase inhibitor ICI 198583 with an undefined mechanism of action. (semanticscholar.org)

Quinazolinone Niementowski quinazoline synthesis Armarego, W. L. F. (1963). (wikipedia.org)
W. L. F. Armarego, A Text Book of Quinazolines , 1963. (hindawi.com)

Quinazoline is an organic compound with the formula C8H6N2. (wikipedia.org)
In the title compound, C 14 H 10 N 2 O 2 S, the benzothia-zole and quinazoline ring systems are essentially planar with maximum deviations of 0.0127 (16) and 0.1588 (15) Å, respectively, and make a dihedral angleof 3.02 (5)°, which shows that the entire mol-ecule is almost planar. (iucr.org)
The title compound comprises a benzothiazole ring fused with quinazoline ring. (iucr.org)

The thiazole ring (C1/C6/C7/N1/S1) forms a dihedral angle of 0.34 (8)° and 3.15 (6)° with the phenyl ring (C1-C6) and the quinazoline ring system, respectively. (iucr.org)
The results of the comprehensive structure-activity relationship study confirmed the assumption that two or more electronegative groups on the phenyl ring attached to the thiazolo[2,3-b]quinazoline system showed the optimum effect. (dovepress.com)
The aldonitrone 1c also reacts with N-methylmaleimide and with phenyl vinyl sulfone to furnish the first examples of primary cycloaddition products from quinazoline 3-oxides. (nuigalway.ie)
In such fashion, in this paper, we report the synthesis and anticonvulsant activity (Chemo shock) of N-1(substituted-N-4[(4-oxo-3-phenyl-3, 4-dihydro-quinazoline-2-ylmethyl) semicarbazones 3A-d (1-7), 3B-d (1-7), 3C-d (1-7), their chemical structure were characterized using IR, H-H NMR, and elemental analysis techniques. (innovareacademics.in)

Nitro, Amino, and Related Quinazolines. (wiley.com)
Amination of the 2-aryl-6-bromo-4-chloro-8-iodoquinazolines with 2-aminoethanol followed by acid-promoted cyclodehydration of the incipient 2-((6,8-dihalo-2-phenylquinazolin-4-yl)amino)ethanols afforded the corresponding novel 5-aryl-9-bromo-7-iodo-2,3-dihydro-2 H -imidazo[1,2- c ]quinazolines. (mdpi.com)
The ''Global and Chinese 4-amino-2-chloro-6,7-dimethoxy quinazoline Industry, 2011-2021 Market Research Report'' is a professional and in-depth study on the current state of the global 4-amino-2-chloro-6,7-dimethoxy quinazoline industry with a focus on the Chinese market. (reportsnreports.com)
The report provides key statistics on the market status of the 4-amino-2-chloro-6,7-dimethoxy quinazoline manufacturers and is a valuable source of guidance and direction for companies and individuals interested in the industry.Firstly, the report provides a basic overview of the industry including its definition, applications and manufacturing technology. (reportsnreports.com)
Through the statistical analysis, the report depicts the global and Chinese total market of 4-amino-2-chloro-6,7-dimethoxy quinazoline industry including capacity, production, production value, cost/profit, supply/demand and Chinese import/export. (reportsnreports.com)
The report then estimates 2016-2021 market development trends of 4-amino-2-chloro-6,7-dimethoxy quinazoline industry. (reportsnreports.com)
In the end, the report makes some important proposals for a new project of 4-amino-2-chloro-6,7-dimethoxy quinazoline Industry before evaluating its feasibility. (reportsnreports.com)
Overall, the report provides an in-depth insight of 2011-2021 global and Chinese 4-amino-2-chloro-6,7-dimethoxy quinazoline industry covering all important parameters. (reportsnreports.com)
5.2 Market Competition of 4-amino-2-chloro-6,7-dimethoxy quinazoline Industry by Country (USA, EU, Japan, Chinese etc. (reportsnreports.com)

The optimal conditions of the reaction have been found, and factors contributing to oxidation of 5-R-2-aryl-5,6-dihydro-[1,2,4]triazolo[1,5-с]quinazolines have been determined. (edu.ua)

The latter were, in turn, subjected to sequential (Sonogashira and Suzuki-Miyaura) and one-pot two-step (Sonogashira/Stille) cross-coupling reactions to afford diversely functionalized polycarbo-substituted 2 H -imidazo[1,2- c ]quinazolines. (mdpi.com)
The iridium and platinum cyclometalated imidazo[1,2- c ]quinazolines have also been patented as efficient dopants for organic electroluminescent layers in organic light emitting diodes (OLEDS) [ 6 ]. (mdpi.com)

The current investigation could be extremely helpful for the development of newer therapeutically useful quinazoline based molecules for cancer therapy. (medworm.com)
The reaction proceeded smoothly under metal-free conditions, which provided quinazoline-containing heterocyclic molecules in moderate to good yields. (rsc.org)

Biotransformation of quinazoline and phthalazine by Aspergillus niger. (sigmaaldrich.com)
Cultures of Aspergillus niger NRRL-599 in fluid Sabouraud medium were grown with quinazoline and phthalazine for 7 days. (sigmaaldrich.com)
Biological Activities of the Alkaloid Quinazoline Extracted from Aspergillus nomius ', Egyptian Journal of Botany , 57(3), pp. 565-582. (ekb.eg)

Quinazoline was oxidized to 4-quinazolinone and 2,4-quinazolinedione, and phthalazine was oxidized to 1-phthalazinone. (sigmaaldrich.com)

Structural studies using X-ray crystallography reveal a new conformation of SIIP and key interactions made by substituents located at the quinazoline 2-, 4-, and 7-positions. (rcsb.org)

In 1903, Siegmund Gabriel reported the synthesis of the parent quinazoline from o-nitrobenzylamine, which was reduced with hydrogen iodide and red phosphorus to 2-aminobenzylamine. (wikipedia.org)

For example, reaction of 2-chloro-4-(4-methylpiperazin-1-yl)quinazoline with N-methyl-4-chlorobenzenesulfonamide gave II in 10% yield. (diva-portal.org)

Quinazoline is a planar molecule. (wikipedia.org)
The quinazoline ring system is also essentially planar with the maximum deviation of -0.1588 (15)Å for the N1 atom. (iucr.org)

The 5-(4-chlorostyryl)-2-phenylimidazo[1,2- c ] quinazoline 2 , on the other hand, was found to exhibit significant anti-cancer activity against HEP-G2 liver cell line [ 5 ]. (mdpi.com)
Quinazoline is a heterocycle and is, for example, a subunit of many anti-cancer drugs. (technologynetworks.com)

A series of new 2, 4-disubstituted quinazolines were synthesized by an analog design approach. (bvsalud.org)

Quinazoline-containing drugs Gefitinib for treatment of non-small-cell lung carcinoma. (wikipedia.org)
As compared with the doses of standard drugs required for cure of infections with drug-susceptible strains or doses of the newly developed aminoalcohols required for cure of either drug-susceptible or drug-resistant strains, each of these quinazolines effected cure of infections with the Oak Knoll strain at a remarkably small daily dose. (ajtmh.org)

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Health Care1

Potency and mechanism of action of E4021, a type 5 phosphodiesterase isozyme-selective inhibitor, on the photoreceptor phosphodiesterase depend on the state of activation of the enzyme. (1/3696)

Interactive effects of inhibitors of poly(ADP-ribose) polymerase and DNA-dependent protein kinase on cellular responses to DNA damage. (2/3696)

A phase I study of the lipophilic thymidylate synthase inhibitor Thymitaq (nolatrexed dihydrochloride) given by 10-day oral administration. (3/3696)

Inhibition of transforming growth factor alpha (TGF-alpha)-mediated growth effects in ovarian cancer cell lines by a tyrosine kinase inhibitor ZM 252868. (4/3696)

Keratinocyte collagenase-1 expression requires an epidermal growth factor receptor autocrine mechanism. (5/3696)

A novel class of lipophilic quinazoline-based folic acid analogues: cytotoxic agents with a folate-independent locus. (6/3696)

Activation-dependent clustering of the erbB2 receptor tyrosine kinase detected by scanning near-field optical microscopy. (7/3696)

Pleiotropic coupling of G protein-coupled receptors to the mitogen-activated protein kinase cascade. Role of focal adhesions and receptor tyrosine kinases. (8/3696)

Quinazolines

PubMed

Periodicals as Topic

Books

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MEDLINE

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Potassium Channels

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Ion Channel Gating

Potassium

Potassium Channels, Voltage-Gated

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Radioligand Assay

Schizophrenia

Receptor, Serotonin, 5-HT2A

Receptors, Serotonin, 5-HT1

Receptor, Serotonin, 5-HT1A

Lewis Acids

Quinazolinones

Cyclization

Chemistry Techniques, Synthetic

Molecular Structure

Scandium

Benzothiazoles

Thiazoles

Sweetening Agents

Saccharin

Folic Acid Antagonists

Heterocyclic Compounds

Cell Cycle

Pathology, Molecular

Cyclin-Dependent Kinases

Cell Cycle Proteins

Molecular Sequence Data

Models, Molecular

Trimetrexate

Thiophenes

Thymidylate Synthase

Television

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Carbon Dioxide

Carbon Footprint

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Models, Chemical

Models, Theoretical

Thermodynamics

Potency and mechanism of action of E4021, a type 5 phosphodiesterase isozyme-selective inhibitor, on the photoreceptor phosphodiesterase depend on the state of activation of the enzyme. (1/3696)

Interactive effects of inhibitors of poly(ADP-ribose) polymerase and DNA-dependent protein kinase on cellular responses to DNA damage. (2/3696)

A phase I study of the lipophilic thymidylate synthase inhibitor Thymitaq (nolatrexed dihydrochloride) given by 10-day oral administration. (3/3696)

Inhibition of transforming growth factor alpha (TGF-alpha)-mediated growth effects in ovarian cancer cell lines by a tyrosine kinase inhibitor ZM 252868. (4/3696)

Keratinocyte collagenase-1 expression requires an epidermal growth factor receptor autocrine mechanism. (5/3696)

A novel class of lipophilic quinazoline-based folic acid analogues: cytotoxic agents with a folate-independent locus. (6/3696)

Activation-dependent clustering of the erbB2 receptor tyrosine kinase detected by scanning near-field optical microscopy. (7/3696)

Pleiotropic coupling of G protein-coupled receptors to the mitogen-activated protein kinase cascade. Role of focal adhesions and receptor tyrosine kinases. (8/3696)

Eldorado: Mental disorder or conscious disturbance in epidermal growth factor receptor-tyrosine kinase inhibitor treatment of...

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MOESM12 of STAT3 induces G9a to exacerbate HER3 expression for the survival of epidermal growth factor receptor-tyrosine kinase...

Design and Synthesis of 4-substituted Quinazolines as Potent EGFR Inhibitors with Anti-breast Cancer Activity | Bentham Science

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The epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 (Iressa) suppresses proliferation and invasion of human...

5,6-Dihydro-[1,2,4]triazolo[1,5-c]quinazolines. Message 1. Features of interactions between [2-(3-aryl-1H-1,2,4-triazole-5-yl...

The prognostic role of EGFR-TKIs for patients with advanced non-small cell lung cancer | Scientific Reports

The peripheral blood neutrophil-to-lymphocyte ratio is a prognostic predictor for survival of EGFR-mutant nonsmall cell lung...

The benefits of achieving stable disease in advanced lung cancer<...

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A randomized, phase II study of gefitinib alone versus nimotuzumab plus gefitinib after platinum-based chemotherapy in advanced...

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Gemcitabine Overcomes Erlotinib Resistance in EGFR-Overexpressing Cancer Cells through Downregulation of Akt [Abstract]

Preparation of piperazinyl quinazolines as 5-HT6 modulators.

The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. - PubMed -...

Quinazolines as potassium ion channel inhibitors - Patent # 8575184 - PatentGenius

Synthesis and evaluation of quinazolines as inhibitors of the bacterial cell division protein FtsZ - Fingerprint - UC Davis

Gefitinib induces apoptosis in human glioma cells by targeting Bad phosphorylation - Semantic Scholar

Cost-Effectiveness Analysis of Afatinib versus Gefitinib for First-Line Treatment of Advanced EGFR-Mutated Advanced Non-Small...

AstraZeneca in-licenses Synairgens SNG001 for asthma in $232M deal - CenterWatch News Online

Slovakia plans to keeping using AstraZeneca despite pause - WTRF

Epithelial-mesenchymal transition (EMT) is normally one particular mechanism of possessed resistance | COX-2 contributes to the...