Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors
文献类型：期刊论文
| 作者 | Zhang, Dengyou3; Ai, Jing2 ; Liang, Zhongjie3; Li, Chunpu3; Peng, Xia2; Ji, YinChun2; Jiang, Hualiang1,3; Geng, Meiyu2; Luo, Cheng3; Liu, Hong3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2012-09-01 |
| 卷号 | 20期号:17页码:5169-5180 |
| 关键词 | Receptor tyrosine kinase c-Met 2-Aminopyridine-3-carboxamide |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2012.07.007 |
| 文献子类 | Article |
| 英文摘要 | A series of 2-aminopyridine-3-carboxamide derivatives against c-Met were designed and synthesized by employing bioisosteric replacement of heterocyclic moieties with the amide bond. The structure-activity relationship (SAR) at various positions of the scaffold was explored. In this study, a promising compound (S)-24o with a c-Met IC50 of 0.022 mu M was identified. The compound exhibited dose-dependent inhibition of the phosphorylation of c-Met as well as downstream signaling in EBC-1 cells. Furthermore, the interactive binding model of (S)-24o with c-Met was elucidated by virtue of a molecular modeling study. (C) 2012 Elsevier Ltd. All rights reserved. |
| WOS关键词 | HEPATOCYTE GROWTH-FACTOR ; RECEPTOR TYROSINE KINASE ; TUMOR-GROWTH ; LUNG-CANCER ; IN-VIVO ; ANTIBODY ; ANTAGONISTS ; POTENT ; DESIGN ; CELL |
| 资助项目 | National Basic Research Program of China[2009CB940903] ; National Basic Research Program of China[2012CB518000] ; National Natural Science Foundation of China[20721003] ; National Natural Science Foundation of China[81025017] ; National S&T Major Projects[2012ZX09103-101-072] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000307828600012 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277976]  |
| 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 药物发现与设计中心 药物化学研究室 |
| 通讯作者 | Geng, Meiyu |
| 作者单位 | 1.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Biol Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Zhang, Dengyou,Ai, Jing,Liang, Zhongjie,et al. Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2012,20(17):5169-5180. |
| APA | Zhang, Dengyou.,Ai, Jing.,Liang, Zhongjie.,Li, Chunpu.,Peng, Xia.,...&Liu, Hong.(2012).Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,20(17),5169-5180. |
| MLA | Zhang, Dengyou,et al."Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 20.17(2012):5169-5180. |
入库方式： OAI收割
来源：上海药物研究所
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