Design,Synthesis,and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-M

来源 :2015年全国药物化学学术会议暨第五届中英药物化学学术会议 | 被引量 : 0次 | 上传用户:ahehehehehe
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  A series of imidazo[1,2-a]pyridine derivatives against c-Met was designed by means of bioisosteric replacement.1 In our study,a selective,potent c-Met inhibitor,A41 was identified,with IC50 values of 3.9 nM against c-Met kinase and 45.0 nM against c-Met-addicted EBC-1 cell proliferation,respectively.
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根据已报道的双环三氮唑类c-Met抑制剂的结构特征,运用传统的药物化学和计算机辅助设计策略,通过生物电子等排原理设计合成了结构新颖的咪唑并[1,2-a]吡啶类c-Met抑制剂[1].其中,47个化合物对c-Met激酶抑制的IC50值小于50 nM.