Design, Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety
查看参考文献19篇
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文摘
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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. |
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来源
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Chemical Research in Chinese Universities
,2015,31(5):766-773 【核心库】
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DOI
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10.1007/s40242-015-5036-z
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关键词
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6,7-Dimethoxyquinazoline derivative
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Diaryl urea scaffold
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Cytotoxic activity
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地址
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Shenyang Pharmaceutical University, Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang, 110016
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语种
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英文 |
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文献类型
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研究性论文 |
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ISSN
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1005-9040 |
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学科
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化学 |
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基金
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Supported by the Program for Innovative Research Team of the Ministry of Education of the People’s Republic of China and Program for Liaoning Innovative Research Team in University, China
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the Liaoning Excellent Talents in University of China
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文献收藏号
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CSCD:5537997
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参考文献 共
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