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Design, Synthesis and Biological Evaluation of Pyridin‐3‐yl pyrimidines as Potent B cr‐ A bl Inhibitors
Author(s) -
Pan Xiaoyan,
Dong Jinyun,
Gao Hongping,
Wang Fang,
Zhang Yanmin,
Wang Sicen,
Zhang Jie
Publication year - 2014
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12272
Subject(s) - chemistry , docking (animal) , stereochemistry , aniline , inhibitory postsynaptic potential , structure–activity relationship , biological activity , breakpoint cluster region , combinatorial chemistry , biochemistry , in vitro , biology , receptor , organic chemistry , medicine , nursing , neuroscience
A series of pyridin‐3‐yl pyrimidines was synthesized and evaluated for their Bcr‐Abl inhibitory and anticancer activity. The preliminary results indicated that some compounds were promising anticancer agents. Compounds A2 , A8, and A9 exhibited potent Bcr‐Abl inhibitory activity, suggesting that aniline containing halogen substituents might be important for biological activity. Molecular docking was carried out to investigate the binding mode of them with Bcr‐Abl. Details of synthesis and SAR studies of these compounds are described.