中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors

文献类型:期刊论文

作者Zhang, Dengyou3; Ai, Jing1; Liang, Zhongjie4; Zhu, Wei3; Peng, Xia1; Chen, Xianjie3; Ji, YinChun1; Jiang, Hualiang2,3; Luo, Cheng3; Geng, Meiyu1
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2013-04-15
卷号23期号:8页码:2408-2413
关键词c-Met EBC-1 cell Tyrosine kinase receptor
ISSN号0960-894X
DOI10.1016/j.bmcl.2013.02.037
文献子类Article
英文摘要A series of novel 5-(benzyloxy)pyridin-2(1H)-ones were designed, synthesized and biologically evaluated for c-Met inhibition. Various amides and benzoimidazoles at C-3 position were investigated. A potent compound 12b with a c-Met IC50 of 12 nM was identified. This compound exhibited potent inhibition of EBC-1 cell associated with c-Met constitutive activation and showed high selectivity for c-Met than other tested 11 kinases. The binding model 12b with c-Met was disclosed by docking analysis. (C) 2013 Elsevier Ltd. All rights reserved.
WOS关键词KINASE INHIBITORS ; DISCOVERY
资助项目National Basic Research Program of China[2009CB940903] ; National Basic Research Program of China[2009 CB918502] ; National Basic Research Program of China[2012CB518005] ; National Natural Science Foundation of China[21021063] ; National Natural Science Foundation of China[91229204] ; National Natural Science Foundation of China[81102461] ; National Natural Science Foundation of China[81025017] ; National S&T Major Projects[2012ZX09103-101-072] ; National S&T Major Projects[2012ZX09301001-007]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000316934000028
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/277654]  
专题药理学第一研究室
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
药物化学研究室
通讯作者Geng, Meiyu
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China;
2.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res,CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China;
4.Soochow Univ, Ctr Syst Biol, Suzhou 215006, Jiangsu, Peoples R China;
推荐引用方式
GB/T 7714
Zhang, Dengyou,Ai, Jing,Liang, Zhongjie,et al. Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2013,23(8):2408-2413.
APA Zhang, Dengyou.,Ai, Jing.,Liang, Zhongjie.,Zhu, Wei.,Peng, Xia.,...&Liu, Hong.(2013).Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,23(8),2408-2413.
MLA Zhang, Dengyou,et al."Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 23.8(2013):2408-2413.

入库方式: OAI收割

来源:上海药物研究所

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