Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors

doi:10.1016/j.ejmech.2016.03.027

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	Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors
	Lu, Dong 1; Shen, Aijun2 ; Liu, Yang 1; Peng, Xia 2; Xing, Weiqiang 1; Ai, Jing2 ; Geng, Meiyu2 ; Hu, Youhong1
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2016-06-10
卷号	115 页码:191-200
关键词	c-Met Benzo[d]oxazol-2(3H)-one-quinolone Molecular hybridization Anti-cancer
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2016.03.027
文献子类	Article
英文摘要	Analysis of the results of studies of docking 1 and 7a with c-Met kinase led to the identification of benzo [d]oxazol-2(3H)-one-quinolone derivatives as potential inhibitors of this enzyme. A molecular hybrid strategy, using a 4-ethoxy-7-substituted-quinoline core and a benzo[d]oxazol-2(3H)-one scaffold, was employed to design members of this family for study as inhibitors of the kinase and proliferation of EBC-1 cells. Most of the substances were found to display good to excellent c-Met kinase inhibitory activities. The results of a structure activity relationship (SAR) study led to the discovery of benzo[d]oxazol-2(3H)-one-quinolone 13, which has IC50 values of 1 nM against c-Met kinase and 5 nM against proliferation of the EBC-1 cell line. (C) 2016 Elsevier Masson SAS. All rights reserved.
资助项目	National Natural Science Foundation of China[81202392] ; National Natural Science Foundation of China[81225022] ; National Natural Science Foundation of China[81402966] ; National Natural Science Foundation of China[81321092] ; National S&T Major Projects[2012ZX09301001-007]
WOS关键词	GROWTH-FACTOR RECEPTOR ; LUNG-CANCER ; RESISTANCE ; POTENT ; IDENTIFICATION ; ASSOCIATION ; DISCOVERY ; DOCKING ; ANALOGS ; SERIES
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:000375360800017
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276004]
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发现与设计中心药物化学研究室
通讯作者	Geng, Meiyu; Hu, Youhong
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Lu, Dong,Shen, Aijun,Liu, Yang,et al. Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2016,115:191-200.
APA	Lu, Dong.,Shen, Aijun.,Liu, Yang.,Peng, Xia.,Xing, Weiqiang.,...&Hu, Youhong.(2016).Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,115,191-200.
MLA	Lu, Dong,et al."Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 115(2016):191-200.