Synthesis and biological evaluation of 3-aryl-4-indolyl-maleimides as potent mutant isocitrate dehydrogenase-1 inhibitors.

Xiaoqi Liu,Yuanyuan Hu,Anhui Gao,Meng Xu,Lixin Gao,Lei Xu,Yubo Zhou,Jianrong Gao,Qing Ye,Jia Li

Bioorganic & Medicinal Chemistry（2019）

引用 9|浏览30

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摘要

•A series of 3-aryl-4-indolylmaleimide IDH1/R132H inhibitors was synthesized.•7a, 7d, 7h, 7i, 7k and 7o showed high inhibition and high selectivity of IDH1/R132H.•7h, 7i and 7k could effectively suppress the production of 2-HG in U87MG cells.•7h could reversed the block that IDH1 mutation induced in TF-1 cell differentiation.

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关键词

3-Aryl-4-indolyl-maleimides,IDH1/R132H inhibitors,Tumor 2-HG,Synthesis

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