Design, synthesis, and biological evaluation of 3-(1 H-1, 2, 3-triazol-1-yl) benzamide derivatives as potent pan Bcr-Abl inhibitors including the threonine315→ …

Y Li, M Shen, Z Zhang, J Luo, X Pan, X Lu…

文献索引：Li, Yupeng; Shen, Mengjie; Zhang, Zhang; Luo, Jinfeng; Pan, Xiaofen; Lu, Xiaoyun; Long, Huoyou; Wen, Donghai; Zhang, Fengxiang; Leng, Fang; Li, Yingjun; Tu, Zhengchao; Ren, Xiaomei; Ding, Ke Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 10033 - 10046

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被引用次数: 18

摘要

A series of 3-(1 H-1, 2, 3-triazol-1-yl) benzamide derivatives were designed and synthesized as new Bcr-Abl inhibitors by using combinational strategies of bioisosteric replacement, scaffold hopping, and conformational constraint. The compounds displayed significant inhibition against a broad spectrum of Bcr-Abl mutants including the gatekeeper T315I and p- loop mutations, which are associated with disease progression in CML. The most potent ...