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

doi:10.1016/j.bmcl.2019.01.018

	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
	Wang, Yueliang 1,2; Xing, Li 3,4; Ji, Yinchun 1; Ye, Jiqing 3,4; Dai, Yang 1; Gu, Wangting 3,4; Ai, Jing 1,5; Song, Zilan 3,4,5
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2019-03-15
卷号	29 期号:6 页码:836-838
关键词	AXL Kinase Pyrazine Cancer
ISSN号	0960-894X
DOI	10.1016/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.
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关键词	RECEPTOR ; EXPRESSION ; FAMILY ; MET
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000458623500014
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/290453]
专题	中国科学院上海药物研究所
通讯作者	Ai, Jing; Song, Zilan
作者单位	1.Chinese Acad Sci, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, 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.Univ Chinese Acad Sci, Beijing 100049, 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.