Article
Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors.
Bioorganic & medicinal chemistry letters - 1 Dec 2017
Zheng Qiangang, Tang Shuai, Fu Xianlei, Chen Ziqi, Ye Yan, Lan Xiaojing, Jiang Lei, Huang Ying, Ding Jian, Geng Meiyu, Huang Min, Wan Huixin
Abstract excerpt
The discovery and optimization of various of indane amides as mutant IDH1 inhibitors via structure-based rational design were reported. The optimal compounds demonstrated both potent inhibition in IDH1R132H enzymatic activity and 2HG production in IDH1 mutant HT1080 cell line, favorable PK properties and great selectivity against IDH1wt and IDH2R140Q.
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