Identification and synthesis of N '-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase

doi:10.1016/j.bmcl.2011.04.064

	Identification and synthesis of N '-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase
	Liang, Zhongjie 1; Zhang, Dengyou 1; Ai, Jing2 ; Chen, Limin 1; Wang, Hengshuai 1; Kong, Xiangqian 1; Zheng, Mingyue1 ; Liu, Hong1 ; Luo, Cheng1,3 ; Geng, Meiyu2
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2011-06-15
卷号	21 期号:12 页码:3749-3754
关键词	c-Met kinase N '-(2-Oxoindolin-3-ylidene)hydrazide Pharmacophore-based virtual screening
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2011.04.064
文献子类	Article
英文摘要	A series of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives were identified as moderately potent inhibitors against c-Met kinase by pharmacophore-based virtual screening and chemical synthesis methods. The structure-activity relationship (SAR) at various positions of the scaffold was investigated and its binding mode with c-Met kinase was analyzed by molecular modeling studies. In this study, two potent compounds D2 and D25, with IC(50) value at 1.3 mu M and 2.2 mu M against c-Met kinase respectively, were identified. Finally, based on the clues extracted from this study, future development for the optimization of this scaffold was discussed. (C) 2011 Elsevier Ltd. All rights reserved.
资助项目	National Natural Science Foundation of China[20972174] ; National Natural Science Foundation of China[81025017] ; National Natural Science Foundation of China[30725046] ; National Natural Science Foundation of China[91029704] ; National Natural Science Foundation of China[21021063] ; State Key Program of Basic Research of China[2009CB918502] ; Shanghai Committee of Science and Technology[10410703900] ; Chinese Academy of Sciences[XDA01040305] ; National Science & Technology Major Project[2009ZX09301-001] ; Guangdong ST Dept.[2010A030100006] ; Program of Shanghai Subject Chief Scientist[10XD1405100]
WOS关键词	INHIBITORS ; DISCOVERY ; PROTEIN ; POTENT
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000291145900050
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278501]
专题	药物化学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发现与设计中心药理学第一研究室
通讯作者	Liu, Hong
作者单位	1.Chinese Acad Sci, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.Soochow Univ, Ctr Syst Biol, Suzhou 215006, Peoples R China; 4.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China
推荐引用方式 GB/T 7714	Liang, Zhongjie,Zhang, Dengyou,Ai, Jing,et al. Identification and synthesis of N '-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(12):3749-3754.
APA	Liang, Zhongjie.,Zhang, Dengyou.,Ai, Jing.,Chen, Limin.,Wang, Hengshuai.,...&Chen, Kaixian.(2011).Identification and synthesis of N '-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(12),3749-3754.
MLA	Liang, Zhongjie,et al."Identification and synthesis of N '-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21.12(2011):3749-3754.