Further SAR studies on 3,5-diamino-7-trifluoromethylquinolines as highly potent tyrosine kinase c-Met inhibitors: efforts to correct hERG inhibition
文献类型：期刊论文
| 作者 | Wang, Yuanxiang2; Ai, Jing1 ; Yue, Jinfeng1; Peng, Xia1; Ji, Yinchun1; Zhao, Ailing2; Gao, Xin1; Wang, Ying1; Chen, Yi1; Liu, Gang2
|
| 刊名 | MEDCHEMCOMM
 |
| 出版日期 | 2012-11 |
| 卷号 | 3期号:11页码:1423-1427 |
| ISSN号 | 2040-2503 |
| DOI | 10.1039/c2md20192e |
| 文献子类 | Article |
| 英文摘要 | A preclinical study on our previously discovered highly potent c-Met inhibitor 1 (zgwatinib) demonstrated its significant toxicity, and a SAR campaign was conducted to finely tune down the hERG inhibition without affecting the c-Met potency. Compounds 11, 12 and 39 stood out as new c-Met inhibitors with IC50 values of <3.0 nM and being nearly inactive against hERG channels. |
| WOS关键词 | FACTOR SCATTER FACTOR ; GROWTH ; CANCER ; METASTASIS ; PHENOTYPE ; BLOCKERS ; CHANNEL ; CELLS |
| 资助项目 | National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program'[2012ZX09103-101-035] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000311186900010 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277888]  |
| 专题 | 神经药理学研究国际科学家工作站 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 药理学第一研究室 |
| 通讯作者 | Gao, Zhaobing |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Synthet Organ & Med Chem Lab, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Yuanxiang,Ai, Jing,Yue, Jinfeng,et al. Further SAR studies on 3,5-diamino-7-trifluoromethylquinolines as highly potent tyrosine kinase c-Met inhibitors: efforts to correct hERG inhibition[J]. MEDCHEMCOMM,2012,3(11):1423-1427. |
| APA | Wang, Yuanxiang.,Ai, Jing.,Yue, Jinfeng.,Peng, Xia.,Ji, Yinchun.,...&Zhang, Ao.(2012).Further SAR studies on 3,5-diamino-7-trifluoromethylquinolines as highly potent tyrosine kinase c-Met inhibitors: efforts to correct hERG inhibition.MEDCHEMCOMM,3(11),1423-1427. |
| MLA | Wang, Yuanxiang,et al."Further SAR studies on 3,5-diamino-7-trifluoromethylquinolines as highly potent tyrosine kinase c-Met inhibitors: efforts to correct hERG inhibition".MEDCHEMCOMM 3.11(2012):1423-1427. |
入库方式： OAI收割
来源：上海药物研究所
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