Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety
文献类型:期刊论文
作者 | Hou Yunlei; Wu Shasha; Ma Longsheng; Bai Jinying; Liu Zijian; Zhao Yanfang |
刊名 | CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
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出版日期 | 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 |
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. |
入库方式: OAI收割
来源:金属研究所
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