Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase

doi:10.1016/j.ejmech.2015.11.042

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	Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase
	Liu, Yang 2; Jin, Shiyu 2; Peng, Xia 1; Lu, Dong 2; Zeng, Limin 2; Sun, Yiming 1; Ai, Jing1 ; Geng, Meiyu1 ; Hu, Youhong2
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2016-01-27
卷号	108 页码:322-333
关键词	Pyridazinone c-Met inhibitor Cyclization strategy Antitumor
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2015.11.042
文献子类	Article
英文摘要	Over activation of c-Met tyrosine kinase is known to promote tumorigenesis and metastasis, as well as to cause therapeutic resistance. Herein we describe the design, synthesis and biological activities of novel, ATP-competitive, c-Met tyrosine kinase inhibitors that are members of the 6-aryl-2-(3-(heteroarylamino) benzyl)pyridazinone family. A structure-activity relationship (SAR) study of these substances led to identification of pyridazinone 19 as a highly selective and potent c-Met tyrosine inhibitor, which displays favorable pharmacokinetic properties in mice and significant antitumor activity against a c-Met driven EBC-1 tumor xenograft. (C) 2015 Elsevier Masson SAS. All rights reserved.
WOS关键词	HEPATOCYTE GROWTH-FACTOR ; BIOLOGICAL EVALUATION ; DISCOVERY ; CANCER ; DESIGN ; RESISTANCE ; ANTIBODY ; EGFR ; SAR ; IDENTIFICATION
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000369191800027
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276173]
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	Ai, Jing; Geng, Meiyu; Hu, Youhong
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 ZuChongZhi Rd, Shanghai 201203, Peoples R China;
推荐引用方式 GB/T 7714	Liu, Yang,Jin, Shiyu,Peng, Xia,et al. Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2016,108:322-333.
APA	Liu, Yang.,Jin, Shiyu.,Peng, Xia.,Lu, Dong.,Zeng, Limin.,...&Hu, Youhong.(2016).Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,108,322-333.
MLA	Liu, Yang,et al."Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 108(2016):322-333.