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Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: Synthesis and SAR study as tyrosine kinase c-Met inhibitors

文献类型：期刊论文

作者Wu, Kui2; Ai, Jing3; Liu, Qiufeng1; Chen, TianTian1; Zhao, Ailing4; Peng, Xia3; Wang, Yuanxiang4; Ji, Yinchun3; Yao, Qizheng2; Xu, Yechun1
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2012-10-15
卷号22期号:20页码:6368-6372
关键词c-Met kinase 3,5-Diamino-7-trifluoroquinoline hERG Antitumor activity Structure-activity relationship (SAR)
ISSN号0960-894X
DOI10.1016/j.bmcl.2012.08.075
文献子类Article
英文摘要Two series of new analogues were designed by replacing the quinoline scaffold of our earlier lead 2 (zgw-atinib) with quinoxaline and pyrido[2,3-d]pyrimidine frameworks. Moderate c-Met inhibitory activity was observed in the quinoxaline series. Among the pyrido[2,3-d]pyrimidine series, compounds 13a-c possessing an O-linkage were inactive, whilst the N-linked analogues 15a-c retained c-Met inhibitory potency. Highest activity was observed in the 3-nitrobenzyl analog 15b that showed an IC50 value of 6.5 nM. Further structural modifications based on this compound were undergoing. (c) 2012 Elsevier Ltd. All rights reserved.
WOS关键词FACTOR SCATTER FACTOR ; GROWTH ; METASTASIS ; PHENOTYPE ; CANCER ; POTENT ; CELLS
资助项目Chinese National Science Foundation for the Distinguished Young Scholars Program[81125021] ; Chinese National Science Foundation for the Innovation Research Group[810 21062] ; National Science & Technology Major Project on Key New Drug Creation and Manufacturing Program[2012ZX09103-101-035] ; National Science & Technology Major Project on Key New Drug Creation and Manufacturing Program[2010ZX09401-401] ; National Science & Technology Major Project on Key New Drug Creation and Manufacturing Program[2012ZX093010 01-007] ; Shanghai Commission of Science and Technology[10JC1417100] ; Shanghai Commission of Science and Technology[10dz1910104] ; Hundred Talents Project of Chinese Academy of Sciences[00000000] ; National Natural Science Foundation of China[81102461] ; National Program on Key Basic Research Project of China[2012CB910704]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000309609500011
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/277910]  
专题药物发现与设计中心
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Yao, Qizheng
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China;
2.China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China;
4.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		 Wu, Kui,Ai, Jing,Liu, Qiufeng,et al. Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: Synthesis and SAR study as tyrosine kinase c-Met inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(20):6368-6372.
APA Wu, Kui.,Ai, Jing.,Liu, Qiufeng.,Chen, TianTian.,Zhao, Ailing.,...&Zhang, Ao.(2012).Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: Synthesis and SAR study as tyrosine kinase c-Met inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(20),6368-6372.
MLA Wu, Kui,et al."Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: Synthesis and SAR study as tyrosine kinase c-Met inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.20(2012):6368-6372.

入库方式： OAI收割

来源：上海药物研究所

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