Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold

doi:10.3390/molecules19022655

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	Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold
	Zhang, Wei 2; Ai, Jing1 ; Shi, Dakuo 3; Peng, Xia 1; Ji, Yinchun 1; Liu, Jian 2; Geng, Meiyu1 ; Li, Yingxia 2
刊名	MOLECULES
	2014-02
卷号	19 期号:2 页码:2655-2673
关键词	c-Met synthesis kinase inhibitor 3-carboxypiperidin-2-one
ISSN号	1420-3049
DOI	10.3390/molecules19022655
文献子类	Article
英文摘要	A series of compounds containing a novel 3-carboxypiperidin-2-one scaffold based on the lead structure BMS-777607 were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against MKN45 cancer cell lines. The results indicated that five compounds exhibited significant inhibitory effect on c-Met with IC50 values of 8.6-81 nM and four compounds showed potent inhibitory activity against MKN45 cell proliferation, with IC(50)s ranging from 0.57-16 mu M.
资助项目	National Program on Key Basic Research Project of China[2012CB910704] ; National Natural Science Foundation[91229205] ; National Natural Science Foundation[81102461] ; National S&T Major Projects[2012ZX09301001-007]
WOS关键词	RECEPTOR TYROSINE KINASE ; STRUCTURE-BASED DESIGN ; CELL LUNG-CANCER ; IDENTIFICATION ; POTENT ; DERIVATIVES ; SERIES ; METASTASIS
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
语种	英语
出版者	MDPI AG
WOS记录号	WOS:000334418200082
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277194]
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
通讯作者	Geng, Meiyu
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China; 3.Ocean Univ China, Sch Pharm, Qingdao 266003, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Wei,Ai, Jing,Shi, Dakuo,et al. Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold[J]. MOLECULES,2014,19(2):2655-2673.
APA	Zhang, Wei.,Ai, Jing.,Shi, Dakuo.,Peng, Xia.,Ji, Yinchun.,...&Li, Yingxia.(2014).Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold.MOLECULES,19(2),2655-2673.
MLA	Zhang, Wei,et al."Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold".MOLECULES 19.2(2014):2655-2673.