Discovery of novel type II c-Met inhibitors based on BMS-777607

doi:10.1016/j.ejmech.2014.04.056

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	Discovery of novel type II c-Met inhibitors based on BMS-777607
	Zhang, Wei 1; Ai, Jing2 ; Shi, Dakuo 3; Peng, Xia 2; Ji, Yinchun 2; Liu, Jian 1; Geng, Meiyu2 ; Li, Yingxia 1
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2014-06-10
卷号	80 页码:254-266
关键词	c-Met Synthesis Kinase inhibitor
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2014.04.056
文献子类	Article
英文摘要	Twenty-two new analogs based on the structure of BMS-777607 were designed, synthesized, and evaluated to determine their biological activities. Compounds bearing a cyclic sulfonamide or alpha-chloropiperidone scaffold exhibited good activity, which may provide a new basis for further structural optimization. Quinoline-containing analogs exhibited better results than did their counterparts with an aminopyrimidine, aminopyridine, or pyrrolopyridine unit. Two analogs, 22d and 22e, stood out as the most potent c-Met inhibitors with IC(50)s of 0.9 and 1.7 nM, respectively. These two compounds were more potent than BMS-777607 in enzymatic inhibition and cell proliferation studies. (C) 2014 Elsevier Masson SAS. All rights reserved.
资助项目	National Program on Key Basic Research Project of China[2012CB910704] ; Natural Science Foundation of China for Innovation Research Group[81021062] ; National Natural Science Foundation[81102461] ; National Natural Science Foundation[91229205] ; National S&T Major Projects[2012ZX09301001-007]
WOS关键词	CANCER-THERAPY ; DERIVATIVES ; RESISTANCE ; DESIGN ; MOIETY
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000337985400024
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277028]
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.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, 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 type II c-Met inhibitors based on BMS-777607[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,80:254-266.
APA	Zhang, Wei.,Ai, Jing.,Shi, Dakuo.,Peng, Xia.,Ji, Yinchun.,...&Li, Yingxia.(2014).Discovery of novel type II c-Met inhibitors based on BMS-777607.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,80,254-266.
MLA	Zhang, Wei,et al."Discovery of novel type II c-Met inhibitors based on BMS-777607".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 80(2014):254-266.