Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold
文献类型：期刊论文
| 作者 | Cui, Hong1; Peng, Xia2; Liu, Jian1; Ma, Chunhua1; Ji, Yinchun2; Zhang, Wei1; Geng, Meiyu2 ; Li, Yingxia1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2016-09-15 |
| 卷号 | 26期号:18页码:4483-4486 |
| 关键词 | c-Met Synthesis Antiproliferative activity |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2016.07.077 |
| 文献子类 | Article |
| 英文摘要 | A series of 2-oxo-1,2-dihydroquinoline-containing c-Met inhibitors were designed, synthesized and evaluated for their in vitro activities targeting c-Met. Most compounds showed high potency against c-Met with IC50 values in the single-digit nM range. Among these compounds, two target compounds, namely 1h and 1n, stood out as the most potent c-Met inhibitors with IC(50)s of 0.6 and 0.7 nM, respectively. And 1a exhibited higher potency than BMS-777607 did with respect to the inhibition of cell proliferation. The introduction of electron-donating substituent was favorable for the activities of the compounds to some extent. Furthermore, molecular docking studies also gave encouraging results that supported this work. (C) 2016 Elsevier Ltd. All rights reserved. |
| 资助项目 | National Natural Science Foundation of China[81402966] ; National Natural Science Foundation of China[81321092] ; National Science and Technology Major Projects[2012ZX09301001-007] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000382263800019 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275890]  |
| 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; Li, Yingxia |
| 作者单位 | 1.Fudan Univ, Sch Pharm, 826 Zhangheng Rd, 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 |
| 推荐引用方式 GB/T 7714 | Cui, Hong,Peng, Xia,Liu, Jian,et al. Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2016,26(18):4483-4486. |
| APA | Cui, Hong.,Peng, Xia.,Liu, Jian.,Ma, Chunhua.,Ji, Yinchun.,...&Li, Yingxia.(2016).Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,26(18),4483-4486. |
| MLA | Cui, Hong,et al."Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 26.18(2016):4483-4486. |
入库方式： OAI收割
来源：上海药物研究所
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