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

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	Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety
其他题名	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
	2015
发表期刊	CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN	1005-9040
卷号	31 期号:5 页码:766-773
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.
其他摘要	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 IC_(50) values of 0.08, 0.09, 0.16 and 0.19 μmol/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.
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
收录类别	CSCD
语种	英语
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]
CSCD记录号	CSCD:5537997
引用统计	被引频次：1[CSCD] [CSCD记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/148090
专题	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.