Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase
文献类型：期刊论文
| 作者 | Liu, Yang2; Jin, Shiyu2; Peng, Xia1; Lu, Dong2; Zeng, Limin2; Sun, Yiming1; Ai, Jing1 ; Geng, Meiyu1; Hu, Youhong2
|
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2016-01-27 |
| 卷号 | 108页码:322-333 |
| 关键词 | Pyridazinone c-Met inhibitor Cyclization strategy Antitumor |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2015.11.042 |
| 文献子类 | Article |
| 英文摘要 | Over activation of c-Met tyrosine kinase is known to promote tumorigenesis and metastasis, as well as to cause therapeutic resistance. Herein we describe the design, synthesis and biological activities of novel, ATP-competitive, c-Met tyrosine kinase inhibitors that are members of the 6-aryl-2-(3-(heteroarylamino) benzyl)pyridazinone family. A structure-activity relationship (SAR) study of these substances led to identification of pyridazinone 19 as a highly selective and potent c-Met tyrosine inhibitor, which displays favorable pharmacokinetic properties in mice and significant antitumor activity against a c-Met driven EBC-1 tumor xenograft. (C) 2015 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | HEPATOCYTE GROWTH-FACTOR ; BIOLOGICAL EVALUATION ; DISCOVERY ; CANCER ; DESIGN ; RESISTANCE ; ANTIBODY ; EGFR ; SAR ; IDENTIFICATION |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000369191800027 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276173]  |
| 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 药物化学研究室 |
| 通讯作者 | Ai, Jing; Geng, Meiyu; Hu, Youhong |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 ZuChongZhi Rd, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Liu, Yang,Jin, Shiyu,Peng, Xia,et al. Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2016,108:322-333. |
| APA | Liu, Yang.,Jin, Shiyu.,Peng, Xia.,Lu, Dong.,Zeng, Limin.,...&Hu, Youhong.(2016).Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,108,322-333. |
| MLA | Liu, Yang,et al."Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 108(2016):322-333. |
入库方式： OAI收割
来源：上海药物研究所
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