Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors

doi:10.1016/j.bmcl.2013.02.037

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	Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors
	Zhang, Dengyou 3; Ai, Jing1 ; Liang, Zhongjie 4; Zhu, Wei 3; Peng, Xia 1; Chen, Xianjie 3; Ji, YinChun 1; Jiang, Hualiang2,3 ; Luo, Cheng3 ; Geng, Meiyu1
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	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
DOI	10.1016/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.
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关键词	KINASE INHIBITORS ; DISCOVERY
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000316934000028
内容类型	期刊论文
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.