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Discovery and structure-activity-relationship study of novel imidazole cyclopropyl amine analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors

文献类型：期刊论文

作者Zheng, Qiangang3; Chen, Ziqi1,2; Wan, Huixin3; Tang, Shuai2; Ye, Yan2,3; Xu, Yuan2,3; Jiang, Lei3; Ding, Jian1,2; Geng, Meiyu1,2; Huang, Min1,2
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2018-12-15
卷号28期号:23-24页码:3808-3812
ISSN号0960-894X
关键词IDH1 inhibitor Imidazole cyclopropyl amine Structure-based rational design
DOI10.1016/j.bmcl.2018.07.002
文献子类Article
英文摘要The discovery and optimization of imidazole cyclopropyl amime analogues 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, moderate liver microsome stability and PK properties.
WOS关键词ACUTE MYELOID-LEUKEMIA ; MUTATIONS ; BLOCK
资助项目National Natural Science Foundation of China[81573464]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
出版者PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号WOS:000453232500042
源URL[http://119.78.100.183/handle/2S10ELR8/279467]  
专题药理学第一研究室
通讯作者Huang, Min; Huang, Ying
作者单位1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Pudong New Area, 555 Zuchongzhi Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China;
3.Shanghai Haihe Phamiaceut Co Ltd, Pudong New Area, 421 Newton Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Zheng, Qiangang,Chen, Ziqi,Wan, Huixin,et al. Discovery and structure-activity-relationship study of novel imidazole cyclopropyl amine analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2018,28(23-24):3808-3812.
APA Zheng, Qiangang.,Chen, Ziqi.,Wan, Huixin.,Tang, Shuai.,Ye, Yan.,...&Huang, Ying.(2018).Discovery and structure-activity-relationship study of novel imidazole cyclopropyl amine analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,28(23-24),3808-3812.
MLA Zheng, Qiangang,et al."Discovery and structure-activity-relationship study of novel imidazole cyclopropyl amine analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 28.23-24(2018):3808-3812.

入库方式： OAI收割

来源：上海药物研究所

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