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O-Linked Triazolotriazines: Potent and Selective c-Met Inhibitors

文献类型：期刊论文

作者Chen, Fang4; Wang, Ying1,5; Ai, Jing1,2,5; Zhan, Zhengsheng4; Lv, Yongcong4; Liang, Zhongjie3; Luo, Cheng3; Mei, Desheng4; Geng, Meiyu1,5; Duan, Wenhu4
刊名CHEMMEDCHEM
出版日期2012-07
卷号7期号:7页码:1276-1285
关键词c-Met selectivity triazolotriazines tyrosine kinase
ISSN号1860-7179
DOI10.1002/cmdc.201200145
文献子类Article
英文摘要The HGF/c-Met signaling pathway mediates a variety of important biological activities, but dysregulation of the pathway is also closely associated with poor prognosis in a wide range of human cancers. c-Met is considered to be among the most promising therapeutic targets for anticancer drug discovery. Herein we report the discovery of a series of O-linked triazolotriazines that show sub-nanomolar inhibition of c-Met activity. Among these new compounds, 6?a exhibits high c-Met inhibitory potency in both enzymatic and cellular assays with great selectivity.
WOS关键词HEPATOCYTE GROWTH-FACTOR ; RECEPTOR TYROSINE KINASE ; CANCER-CELLS ; LUNG-CANCER ; INVASIVE GROWTH ; SCATTER-FACTOR ; RESISTANCE ; AMPLIFICATION ; METASTASIS ; DISCOVERY
资助项目National Natural Science Foundation[81102461] ; National Natural Science Foundation[81021062] ; National Natural Science Foundation[90813034] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program" of the People's Republic of China[2012ZX09301-001-007] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program" of the People's Republic of China[2012ZX09103101-024] ; Shanghai Science and Technology Commission[11431921100]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000305604100016
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/278031]  
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Chen, Fang
作者单位1.Chinese Acad Sci, Div Antitumor Pharmacol, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
2.Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210032, Jiangsu, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China;
5.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Chen, Fang,Wang, Ying,Ai, Jing,et al. O-Linked Triazolotriazines: Potent and Selective c-Met Inhibitors[J]. CHEMMEDCHEM,2012,7(7):1276-1285.
APA Chen, Fang.,Wang, Ying.,Ai, Jing.,Zhan, Zhengsheng.,Lv, Yongcong.,...&Duan, Wenhu.(2012).O-Linked Triazolotriazines: Potent and Selective c-Met Inhibitors.CHEMMEDCHEM,7(7),1276-1285.
MLA Chen, Fang,et al."O-Linked Triazolotriazines: Potent and Selective c-Met Inhibitors".CHEMMEDCHEM 7.7(2012):1276-1285.

入库方式： OAI收割

来源：上海药物研究所

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