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Discovery of a potent tyrosine kinase AXL inhibitor bearing the 3-((2,3,4,5-tetrahydro-1H-benzo [d] azepin-7-yl)amino)pyrazine core

文献类型：期刊论文

作者Wang, Yueliang2,5; Xing, Li3,4; Ji, Yinchun5; Ye, Jiqing3,4; Dai, Yang5; Gu, Wangting3,4; Ai, Jing1,5; Song, Zilan1,3,4
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2019-03-15
卷号29期号:6页码:836-838
关键词AXL Kinase Pyrazine Cancer
ISSN号0960-894X
DOI10.1016/j.bmcl.2019.01.018
通讯作者Ai, Jing(jai@simm.ac.cn) ; Song, Zilan(songalan@simm.ac.cn)
英文摘要Starting from the recently launched FLT3/AXL multi-targeted inhibitor Gilteritinib (5), we conducted a side-chain ring closure medicinal chemistry approach leading to the identification of compound 15c as a highly potent AXL inhibitor in the biochemical and cellular anti-proliferative assays, with IC50 values of 1.2 and 0.3 nM, respectively. Compared with the reference compound 5, our new discovered AXL inhibitor 15c is more potent in both assays.
WOS关键词RECEPTOR ; EXPRESSION ; FAMILY ; MET
资助项目National Natural Science Foundation of China[81773762] ; National Natural Science Foundation of China[81703327] ; Shanghai Commission of Science and Technology[17431902900]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000458623500014
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/290453]  
专题新药研究国家重点实验室
通讯作者Ai, Jing; Song, Zilan
作者单位1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
2.Shanghai Univ, Shanghai Key Lab Bioenergy Crops, Sch Life Sci, Shanghai 200444, Peoples R China
3.Chinese Acad Sci, CAS Key Lab Receptor Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
4.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
5.Chinese Acad Sci, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Yueliang,Xing, Li,Ji, Yinchun,et al. Discovery of a potent tyrosine kinase AXL inhibitor bearing the 3-((2,3,4,5-tetrahydro-1H-benzo [d] azepin-7-yl)amino)pyrazine core[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2019,29(6):836-838.
APA Wang, Yueliang.,Xing, Li.,Ji, Yinchun.,Ye, Jiqing.,Dai, Yang.,...&Song, Zilan.(2019).Discovery of a potent tyrosine kinase AXL inhibitor bearing the 3-((2,3,4,5-tetrahydro-1H-benzo [d] azepin-7-yl)amino)pyrazine core.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,29(6),836-838.
MLA Wang, Yueliang,et al."Discovery of a potent tyrosine kinase AXL inhibitor bearing the 3-((2,3,4,5-tetrahydro-1H-benzo [d] azepin-7-yl)amino)pyrazine core".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 29.6(2019):836-838.

入库方式： OAI收割

来源：上海药物研究所

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