Identification and synthesis of N '-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase
文献类型：期刊论文
| 作者 | Liang, Zhongjie1; Zhang, Dengyou1; Ai, Jing2 ; Chen, Limin1; Wang, Hengshuai1; Kong, Xiangqian1; Zheng, Mingyue1; Liu, Hong1; Luo, Cheng1,3; Geng, Meiyu2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 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. |
| WOS关键词 | INHIBITORS ; DISCOVERY ; PROTEIN ; POTENT |
| 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研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000291145900050 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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