Design and synthesis of 3,3 '-biscoumarin-based c-Met inhibitors

doi:10.1039/c4ob00364k

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	Design and synthesis of 3,3 '-biscoumarin-based c-Met inhibitors
	Xu, Jimin 1; Ai, Jing2 ; Liu, Sheng 1; Peng, Xia 2; Yu, Linqian 1; Geng, Meiyu2 ; Nan, Fajun1
刊名	ORGANIC & BIOMOLECULAR CHEMISTRY
	2014
卷号	12 期号:22 页码:3721-3734
ISSN号	1477-0520
DOI	10.1039/c4ob00364k
文献子类	Article
英文摘要	A library of biscoumarin-based c-Met inhibitors was synthesized, based on optimization of 3,3'-biscoumarin hit 3, which was identified as a non-ATP competitive inhibitor of c-Met from a diverse library of coumarin derivatives. Among these compounds, 38 and 40 not only showed potent enzyme activities with IC50 values of 107 nM and 30 nM, respectively, but also inhibited c-Met phosphorylation in BaF3/TPR-Met and EBC-1 cells.
资助项目	National Natural Science Foundation of China[30725049] ; National Natural Science Foundation of China[81321092] ; National Natural Science Foundation of China[81102461] ; National Natural Science Foundation of China[91229205] ; National Science and Technology Major Projects for Major New Drugs Innovation and Development[2012ZX09304011] ; National Program on Key Basic Research Project of China[2012CB910704] ; National S&T Major Projects[2012ZX09301001-007]
WOS关键词	HEPATOCYTE GROWTH-FACTOR ; MONOCLONAL-ANTIBODIES ; ORGANIC-SYNTHESIS ; CELL CARCINOMA ; IN-VIVO ; CANCER ; OVEREXPRESSION ; DERIVATIVES ; 4-HYDROXYCOUMARIN ; MECHANISMS
WOS研究方向	Chemistry
语种	英语
出版者	ROYAL SOC CHEMISTRY
WOS记录号	WOS:000336782000026
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277287]
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国家新药筛选中心
通讯作者	Geng, Meiyu
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Chinese Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Xu, Jimin,Ai, Jing,Liu, Sheng,et al. Design and synthesis of 3,3 '-biscoumarin-based c-Met inhibitors[J]. ORGANIC & BIOMOLECULAR CHEMISTRY,2014,12(22):3721-3734.
APA	Xu, Jimin.,Ai, Jing.,Liu, Sheng.,Peng, Xia.,Yu, Linqian.,...&Nan, Fajun.(2014).Design and synthesis of 3,3 '-biscoumarin-based c-Met inhibitors.ORGANIC & BIOMOLECULAR CHEMISTRY,12(22),3721-3734.
MLA	Xu, Jimin,et al."Design and synthesis of 3,3 '-biscoumarin-based c-Met inhibitors".ORGANIC & BIOMOLECULAR CHEMISTRY 12.22(2014):3721-3734.