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Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety
Alternative TitleDesign, 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 PublicationCHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN1005-9040
Volume31Issue:5Pages:766-773
AbstractA 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 AbstractA 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.
KeywordRECEPTOR TYROSINE KINASES BIOLOGICAL EVALUATION HIGHLY POTENT INHIBITOR IDENTIFICATION GROWTH DISCOVERY SORAFENIB EGFR 6,7-Dimethoxyquinazoline derivative Diaryl urea scaffold Cytotoxic activity
Indexed ByCSCD
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 IDCSCD:5537997
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Document Type期刊论文
Identifierhttp://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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