| Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety | |
| Alternative Title | 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 | |
| Source Publication | CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
 |
| ISSN | 1005-9040 |
| Volume | 31Issue:5Pages:766-773 |
| Abstract | 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. |
| Other Abstract | 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. |
| Keyword | RECEPTOR TYROSINE KINASES BIOLOGICAL EVALUATION HIGHLY POTENT INHIBITOR IDENTIFICATION GROWTH DISCOVERY SORAFENIB EGFR 6,7-Dimethoxyquinazoline derivative Diaryl urea scaffold Cytotoxic activity |
| Indexed By | CSCD |
| Language | 英语 |
| Funding Project | [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 ID | CSCD:5537997 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.imr.ac.cn/handle/321006/148090 |
| Collection | 中国科学院金属研究所 |
| Affiliation | 中国科学院金属研究所 |
| Recommended Citation 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. |
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