Scaffold Hopping-Driven Optimization of 4-(Quinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)-ones as Novel Tubulin Inhibitors
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چکیده
منابع مشابه
Synthesis and Antimicrobial Activity of 3-(1,3,4-Oxadiazol-2-yl)quinazolin-4(3H)-ones
In attempt to find new pharmacologically active molecules, we report here the synthesis and in vitro antimicrobial activity of various 3-(1,3,4-oxadiazol-2-yl)-quinazolin-4(3H)-ones. The antimicrobial activity of title compounds were examined against two gram positive bacteria (S. aureus, S. pyogenes), two gram negative bacteria (E. coli, P. aeruginosa) and three fungi (C. albicans, A. niger, A...
متن کاملThe Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists.
We herein describe the rapid synthesis of a diverse set of dihydroquinazolin-4-ones and quinazolin-4-ones, their biological evaluation as thyroid stimulating hormone receptor (TSHR) agonists, and SAR analysis. Among the compounds screened, 8b was 60-fold more potent than the hit compound 1a, which was identified from a high throughput screen of over 73,000 compounds.
متن کاملSynthesis and Antimicrobial Evaluation of New (4-Oxo-thiazolidinyl)quinazolin-4(3H)ones of 2-[(2,6-Dichlorophenyl)amino]phenylacetic acid
Synthesis of 2-[2-(2,6-dichlorophenyl)amino]phenylmethyl-3-[4-(2-substitutedphenyl-4-oxo-thiazolidinyl)aryl]-6-bromo quinazolin-4(3H)ones VIa-j have been achieved from the starting material 2-[(2,6-dichlorophenyl)amino] phenylacetic acid I to benzoxazine III, Further reaction with p-phenylindiamine and substituted aromatic aldehyde gave 2-[2-(2,6-dichlorophenyl)amino]phenyl methyl-3-(4-aminoary...
متن کاملSynthesis and Antimicrobial Evaluation of New (4-Oxo-thiazolidinyl)quinazolin-4(3H)ones of 2-[(2,6-Dichlorophenyl)amino]phenylacetic acid
Synthesis of 2-[2-(2,6-dichlorophenyl)amino]phenylmethyl-3-[4-(2-substitutedphenyl-4-oxo-thiazolidinyl)aryl]-6-bromo quinazolin-4(3H)ones VIa-j have been achieved from the starting material 2-[(2,6-dichlorophenyl)amino] phenylacetic acid I to benzoxazine III, Further reaction with p-phenylindiamine and substituted aromatic aldehyde gave 2-[2-(2,6-dichlorophenyl)amino]phenyl methyl-3-(4-aminoary...
متن کاملSynthesis and microbial studies of (4-oxo-thiazolidinyl) sulfonamides bearing quinazolin-4(3H)ones.
2-[(2,6-Dichlorophenyl)amino]phenylacetic acid (A) on reaction with thionyl chloride gave corresponding acid chloride (B). A series of (4-oxo-thiazolidinyl)sulfonamides of quinazolin-4(3H)ones (4a-l) were prepared from Schiff bases (3a-l) of 2-[2-(2,6-dichlorophenyl)amino]phenylmethyl-3-[(4-aminophenyl)sulfonamido-1-yl]quinazolin-4(3H)one (D) and substituted aromatic aldehyde. Newly synthesized...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2019
ISSN: 1948-5875,1948-5875
DOI: 10.1021/acsmedchemlett.9b00352