Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors
文献类型：期刊论文
| 作者 | Zheng, Qiangang1; Tang, Shuai2; Fu, Xianlei1; Chen, Ziqi2; Ye, Yan1,2; Lan, Xiaojing2 ; Jiang, Lei1; Huang, Ying1; Ding, Jian2; Geng, Meiyu2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2017-12-01 |
| 卷号 | 27期号:23页码:5262-5266 |
| 关键词 | IDH1 inhibitor Indane amide Structure-based rational design |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2017.10.029 |
| 文献子类 | Article |
| 英文摘要 | 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 IDH1(R132H) enzymatic activity and 2HG production in IDH1 mutant HT1080 cell line, favorable PK properties and great selectivity against IDH1(wt) and IDH2(R140Q). (C) 2017 Elsevier Ltd. All rights reserved. |
| WOS关键词 | ACUTE MYELOID-LEUKEMIA ; MUTATIONS ; GLIOMAS |
| 资助项目 | China International Science and Technology Cooperation Program[2015DFM30040] ; National Natural Science Foundation of China[81573464] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000415643400032 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272380]  |
| 专题 | 药理学第一研究室 |
| 通讯作者 | Huang, Min; Wan, Huixin |
| 作者单位 | 1.Shanghai Haihe Pharmaceut Co Ltd, 421 Newton Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, 555 Zuchongzhi Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zheng, Qiangang,Tang, Shuai,Fu, Xianlei,et al. Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2017,27(23):5262-5266. |
| APA | Zheng, Qiangang.,Tang, Shuai.,Fu, Xianlei.,Chen, Ziqi.,Ye, Yan.,...&Wan, Huixin.(2017).Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,27(23),5262-5266. |
| MLA | Zheng, Qiangang,et al."Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 27.23(2017):5262-5266. |
入库方式： OAI收割
来源：上海药物研究所
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