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Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors |
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| Authors: | Qiangang Zheng Shuai Tang Xianlei Fu Ziqi Chen Yan Ye Xiaojing Lan Lei Jiang Ying Huang Jian Ding Meiyu Geng Min Huang Huixin Wan |
| Affiliation: | 1. Shanghai Haihe Pharmaceutical, Co., Ltd., 421 Newton Road, Zhangjiang Hi-tech Park, Pudong New Area, Shanghai 201203, China;2. Shanghai Institute of Materia Medica, Chinese Academy of Science, 555 Zuchongzhi Road, Zhangjiang Hi-tech Park, Pudong New Area, Shanghai 201203, China |
| Abstract: | 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. |
| Keywords: | IDH1 inhibitor Indane amide Structure-based rational design |
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