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3-(7-Azaindolyl)-4-indolylmaleimides as a novel class of mutant isocitrate dehydrogenase-1 inhibitors: Design, synthesis, and biological evaluation

文献类型：期刊论文

作者Hu, Yuanyuan1; Gao, Anhui3; Liao, Honghui2; Zhang, Mengmeng3; Xu, Gaoya3; Gao, Lixin3; Xu, Lei3; Zhou, Yubo3; Gao, Jianrong1; Ye, Qing1
刊名ARCHIV DER PHARMAZIE
出版日期2018-10
卷号351期号:10
关键词2-hydroxyglutaric acid 3-(7-azaindoyl)-4-indolylmaleimides isocitrate dehydrogenase 1 inhibitors tumor
ISSN号0365-6233
DOI10.1002/ardp.201800039
文献子类Article
英文摘要A series of 3-(7-azainodyl)-4-indolylmaleimides was designed, synthesized, and evaluated for their isocitrate dehydrogenase 1 (IDH1)/R132H inhibitory activities. Many compounds such as 11a, 11c, 11e, 11g, and 11s exhibited favorable inhibitory effects on IDH1/R132H and were highly selective against the wild-type IDH1. Evaluation of the biological activities at the cellular level showed that compounds 11a, 11c, 11e, 11g, and 11s could effectively suppress the production of 2-hydroxyglutaric acid in U87MG cells expressing IDH1/R132H. Preliminary structure-activity relationship (SAR) and molecular modeling studies were discussed based on the experimental data obtained. These findings may provide new insights into the development of novel IDH1/R132H inhibitors.
WOS关键词ACUTE MYELOID-LEUKEMIA ; 2 MUTATIONS ; SELECTIVE-INHIBITION ; IDH2 MUTATIONS ; IN-VIVO ; GLIOMA ; POTENT ; CELLS ; 2-HYDROXYGLUTARATE ; LEUKEMOGENESIS
资助项目China Postdoctoral Science Foundation[2014M550256] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020328] ; Open Fund of State Key Laboratory of New Drugs, Shanghai Institute of Materia Medica, Chinese Academy of Sciences[SIMM1601KF-04] ; Personalized Medicines-Molecular Signature-based Drug Discovery and Development[00000000] ; Natural Science Foundation of Zhejiang Province[LY18H300009] ; National Natural Science Foundation of China[8150131067]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000446308600001
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/279560]  
专题国家新药筛选中心
中科院受体结构与功能重点实验室
新药研究国家重点实验室
药物安全性评价中心
通讯作者Ye, Qing; Li, Jia
作者单位1.Zhejiang Univ Technol, State Key Lab Breeding Base Green Chem Synth Tech, Hangzhou 310032, Zhejiang, Peoples R China;
2.Second People Hosp Xihu Dist, Hangzhou, Zhejiang, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Hu, Yuanyuan,Gao, Anhui,Liao, Honghui,et al. 3-(7-Azaindolyl)-4-indolylmaleimides as a novel class of mutant isocitrate dehydrogenase-1 inhibitors: Design, synthesis, and biological evaluation[J]. ARCHIV DER PHARMAZIE,2018,351(10).
APA Hu, Yuanyuan.,Gao, Anhui.,Liao, Honghui.,Zhang, Mengmeng.,Xu, Gaoya.,...&Li, Jia.(2018).3-(7-Azaindolyl)-4-indolylmaleimides as a novel class of mutant isocitrate dehydrogenase-1 inhibitors: Design, synthesis, and biological evaluation.ARCHIV DER PHARMAZIE,351(10).
MLA Hu, Yuanyuan,et al."3-(7-Azaindolyl)-4-indolylmaleimides as a novel class of mutant isocitrate dehydrogenase-1 inhibitors: Design, synthesis, and biological evaluation".ARCHIV DER PHARMAZIE 351.10(2018).

入库方式： OAI收割

来源：上海药物研究所

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