Design, Synthesis and Biological Evaluation of Pyridin??3??yl pyrimidines as Potent Bcr??Abl Inhibitors

X Pan, J Dong, H Gao, F Wang, Y Zhang…

Index: Pan, Xiaoyan; Dong, Jinyun; Gao, Hongping; Wang, Fang; Zhang, Yanmin; Wang, Sicen; Zhang, Jie Chemical Biology and Drug Design, 2014 , vol. 83, # 5 p. 592 - 599

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Citation Number: 6

Abstract

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 ...