中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
  4. 药理学第一研究室
Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors

文献类型：期刊论文

作者Liu, Zhiqing1; Yue, Xihua2; Song, Zilan1; Peng, Xia2; Guo, Junfeng1; Ji, Yinchun2; Cheng, Zhen3; Ding, Jian2; Ai, Jing2; Geng, Meiyu2
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2014-10-30
卷号86页码:438-448
关键词2-Aminothiazole ALK kinase Gatekeeper mutation 2,4-Diarylaminopyrimidine Non-small-cell lung cancer
ISSN号0223-5234
DOI10.1016/j.ejmech.2014.09.003
文献子类Article
英文摘要A series of new 2,4-diarylaminopyrimidine analogues (DAAPalogues) was developed by incorporation of a substituted 2-aminothiazole component as the C-2 substituent of the center pyrimidine core. Compound 5i showed highest potency of 12.4 nM against ALK and 24.1 nM against ALK gatekeeper mutation L1196M. Although only having moderate cellular potency in the SUP-M2 cells harboring NPM-ALK, compound 5i showed good kinase selectivity and dose-dependently inhibited phosphorylation of ALK and its down-stream signaling pathways. (C) 2014 Elsevier Masson SAS. All rights reserved.
WOS关键词LUNG-CANCER ; FUSION ; GENE ; NPM
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Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000343781800039
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/276864]  
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Geng, Meiyu
作者单位1.Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Synthet Organ & Med Chem Lab, Shanghai 201203, Peoples R China;
2.Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China;
3.Stanford Univ, Sch Med, Dept Radiol, Mol Imaging Program Stanford,Bio X Program, Stanford, CA 94305 USA
推荐引用方式
GB/T 7714		 Liu, Zhiqing,Yue, Xihua,Song, Zilan,et al. Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,86:438-448.
APA Liu, Zhiqing.,Yue, Xihua.,Song, Zilan.,Peng, Xia.,Guo, Junfeng.,...&Zhang, Ao.(2014).Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,86,438-448.
MLA Liu, Zhiqing,et al."Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 86(2014):438-448.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。