Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety

CORC > 金属研究所 > 中国科学院金属研究所

	Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety
	Hou Yunlei; Wu Shasha; Ma Longsheng; Bai Jinying; Liu Zijian; Zhao Yanfang
刊名	CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
	2015
卷号	31 期号:5 页码:766-773
关键词	RECEPTOR TYROSINE KINASES BIOLOGICAL EVALUATION HIGHLY POTENT INHIBITOR IDENTIFICATION GROWTH DISCOVERY SORAFENIB EGFR 6,7-Dimethoxyquinazoline derivative Diaryl urea scaffold Cytotoxic activity
ISSN号	1005-9040
其他题名	Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety
英文摘要	A series of 6,7-dimethoxyquinazoline derivatives connected by diaryl urea scaffolds was designed, synthesized and their in vitro antitumor activities were evaluated. Most of them showed an excellent potency against the four tested cancer cell lines as compared with sorafenib. Particularly, a promising compound 20 was identified, which showed the most potent antitumor activities with IC50 values of 0.08, 0.09, 0.16 and 0.19 mu mol/L against H460, HT-29, MKN-45 and MDA-MB-231 cell lines, respectively. The structure-activity relationship(SAR) analysis indicated that compounds with dimethylamino or diethylamino group at the C4 position of 6,7-dimethoxyquinazoline moiety exhibited superior activities than compounds bearing morpholino groups.
资助项目	[Program for Innovative Research Team of the Ministry of Education of the People's Republic of China] ; [Program for Liaoning Innovative Research Team in University, China] ; [Liaoning Excellent Talents in University of China]
语种	英语
CSCD记录号	CSCD:5537997
内容类型	期刊论文
源URL	[http://ir.imr.ac.cn/handle/321006/148089]
专题	金属研究所_中国科学院金属研究所
作者单位	中国科学院金属研究所
推荐引用方式 GB/T 7714	Hou Yunlei,Wu Shasha,Ma Longsheng,et al. Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2015,31(5):766-773.
APA	Hou Yunlei,Wu Shasha,Ma Longsheng,Bai Jinying,Liu Zijian,&Zhao Yanfang.(2015).Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,31(5),766-773.
MLA	Hou Yunlei,et al."Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 31.5(2015):766-773.