93246-58-3

Upstream product

• 77206-97-4 2-nitro-5-fluorobenzamide 
• 394-02-5 5-fluoro-2-nitrobenzoyl chloride 
• 320-98-9 5-fluoro-2-nitrobenzoic acid 
• 455-38-9 3-fluorobenzoic acid 
• 2516-95-2 5-chloro-2-nitrobenzoic acid 
• 40763-96-0 2-nitro-5-chlorobenzamide 
• 404009-38-7 2-nitro-5-(1-morpholino)-benzamide 
• 733806-19-4 5-morpholino-2-nitrobenzonitrile 
• 41994-44-9 5-chloro-2-nitrobenzoyl chloride 

Downstream Products

• 733806-36-5 6-methylpyridine-2-carboxylic acid (2-carbamoyl-4-(morpholin-1-yl)phenyl)amide 
• 1253732-02-3 2-{4-[2-(tert-butyl-dimethyl-silanyloxy)-ethoxy]-3,5-dimethyl-phenyl}-6-morpholin-4-yl-3H-quinazolin-4-one 

Relevant academic research and scientific papers

2-((3,5-Dinitrobenzyl)thio)quinazolinones: Potent Antimycobacterial Agents Activated by Deazaflavin (F420)-Dependent Nitroreductase (Ddn)

Swapping the substituents in positions 2 and 4 of the previously synthesized but yet undisclosed 5-cyano-4-(methylthio)-2-arylpyrimidin-6-ones 4, ring closure, and further optimization led to the identification of the potent antitubercular 2-thio-substituted quinazolinone 26. Structure-activity relationship (SAR) studies indicated a crucial role for both meta-nitro substituents for antitubercular activity, while the introduction of polar substituents on the quinazolinone core allowed reduction of bovine serum albumin (BSA) binding (63c, 63d). While most of the tested quinazolinones exhibited no cytotoxicity against MRC-5, the most potent compound 26 was found to be mutagenic via the Ames test. This analogue exhibited moderate inhibitory potency against Mycobacterium tuberculosis thymidylate kinase, the target of the 3-cyanopyridones that lies at the basis of the current analogues, indicating that the whole-cell antimycobacterial activity of the present S-substituted thioquinazolinones is likely due to modulation of alternative or additional targets. Diminished antimycobacterial activity was observed against mutants affected in cofactor F420 biosynthesis (fbiC), cofactor reduction (fgd), or deazaflavin-dependent nitroreductase activity (rv3547), indicating that reductive activation of the 3,5-dinitrobenzyl analogues is key to antimycobacterial activity.

Molecular modelling, synthesis, cytotoxicity and anti-tumour mechanisms of 2-aryl-6-substituted quinazolinones as dual-targeted anti-cancer agents

Background and Purpose Our previous study demonstrated that 6-(pyrrolidin-1-yl)-2-(3-methoxyphenyl)quinazolin-4-one (HMJ38) was a potent anti-tubulin agent. Here, HMJ38 was used as a lead compound to develop more potent anti-cancer agents and to examine t

2-Aryl-4-Quinazolinones And Their Pharmaceutical Compositions

Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R6, R7, R8, R1′, R2′, R3′, R4

NOVEL ANTI-INFLAMMATORY AGENTS

Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.

CONDENSED PYRIDINES AND PYRIMIDINES AND THEIR USE AS ALK-5 RECEPTOR LIGANDS

Therapeutically active substituted quinoline and quinazoline compounds derivatives of formula (I) wherein X is N or CH, Y is NH, N (alkyl) or NH-CH2, and R2 and R3 are specified heterorings, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterised by overexpression of transforming growth factor β (TGF-β), and pharmaceutical compositions for use in such therapy are disclosed.

Synthesis and preliminary cytotoxic and antifungal evaluation of some 6-N,N-dialkyl 2-aryl-4(3H)-quinazolinone derivatives

Some new 2-aryl-4-quinazolinone derivatives bearing a cyclic amino group at position 6 were prepared and their preliminary cytotoxic and antifungal evaluation is reported. They all showed a moderate cytotoxicity suggesting that not only the oxidation stat

6-alkylamino- and 2,3-dihydro-3′-methoxy-2-phenyl-4-quinazolinones and related compounds: Their synthesis, cytotoxicity, and inhibition of tubulin polymerization

As part of our continuing search for potential anticancer candidates among 2-phenyl-4-quinolones and 2-phenyl-4-quinazolinones, two series of 6,7,2′,3′,4′,5′-substituted 2-phenyl-4-quinazolinones and 6,2′,3′,4′,5′-substituted 2,3-dihydro-2-phenyl-4-quinazolinones were synthesized and evaluated for cytotoxicity and as inhibitors of tubulin polymerization. In general, a good correlation was found between the two activities. Five of the 6-substituted heterocyclic 2-phenyl-4-quinozolinones (37-51) showed significant cytotoxicity against a panel of human tumor cell lines with EC50 values in the low micromolar to nanomolar concentration ranges. Compound 38 was the most potent of these compounds, as well as the most potent inhibitor of tubulin polymerization in this series. The activity of 38 was in the same range as those of the antimitotic natural products, colchicine, podophyllotoxin, and combretastatin A-4. Substituted 2-phenyl-4-quinazolinones and 2,3-dihydro-2-phenyl-4-quinazolinones also displayed highly selective cytotoxicity against the ovarian cancer 1A9 and P-gp resistant KB-VIN cell lines.