Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d] isoxazole or 3-aminoindazole scaffold
文献类型：期刊论文
| 作者 | Jiang, Xiaolong1; Liu, Hongyan2; Song, Zilan3; Peng, Xia2; Ji, Yinchun2; Yao, Qizheng1; Geng, Meiyu2 ; Ai, Jing2; Zhang, Ao3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-02-01 |
| 卷号 | 23期号:3页码:564-578 |
| 关键词 | c-Met kinase Inhibitor 3-Amino-benzo[d]isoxazole 3-Aminoindazole Non-small cell lung cancer |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2014.12.002 |
| 文献子类 | Article |
| 英文摘要 | A series of 3-amino-benzo[d]isoxazole-/3-aminoindazole-based compounds were designed, synthesized and pharmacologically evaluated as tyrosine kinase c-Met inhibitors. The SAR study was conducted leading to identification of nine compounds (8d, 8e, 12, 28a-d, 28h and 28i) with IC(50)s less than 10 nM against c-Met. Compound 28a stood out as the most potent c-Met inhibitor displaying potent inhibitory effects both at enzymatic (IC50 = 1.8 nM) and cellular (IC50 = 0.18 mu M on EBC-1 cells) levels. In addition, 28a had a relatively good selectivity compared to a panel of our in-house 14 RTKs. (C) 2014 Elsevier Ltd. All rights reserved. |
| WOS关键词 | FACTOR SCATTER FACTOR ; MEDULLARY-THYROID CANCER ; SIGNALING PATHWAY ; CABOZANTINIB XL184 ; CYTOTOXIC ACTIVITY ; GROWTH ; RECEPTOR ; METASTASIS ; PHENOTYPE ; DRUG |
| 资助项目 | Chinese NSF[81125021] ; Chinese NSF[81373277] ; Chinese NSF[81430080] ; Chinese NSF[81102461] ; Chinese NSF[91229205] ; Chinese NSF[81321092] ; National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program', China[2012ZX09103-101-035] ; National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program', China[2012ZX09301001-007] ; National Program on Key Basic Research Project of China[2012CB910704] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000348039700020 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276659]  |
| 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 | Yao, Qizheng |
| 作者单位 | 1.China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Synthet Organ & Med Chem Lab, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jiang, Xiaolong,Liu, Hongyan,Song, Zilan,et al. Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d] isoxazole or 3-aminoindazole scaffold[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(3):564-578. |
| APA | Jiang, Xiaolong.,Liu, Hongyan.,Song, Zilan.,Peng, Xia.,Ji, Yinchun.,...&Zhang, Ao.(2015).Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d] isoxazole or 3-aminoindazole scaffold.BIOORGANIC & MEDICINAL CHEMISTRY,23(3),564-578. |
| MLA | Jiang, Xiaolong,et al."Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d] isoxazole or 3-aminoindazole scaffold".BIOORGANIC & MEDICINAL CHEMISTRY 23.3(2015):564-578. |
入库方式： OAI收割
来源：上海药物研究所
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