Design,Synthesis and Antitumor Activity of Novel 6,7-Dimethoxyquinazoline Derivatives Containing Diaryl Urea Moiety |
| |
Authors: | HOU Yunlei WU Shasha MA Longsheng BAI Jinying LIU Zijian ZHAO Yanfang |
| |
Affiliation: | Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China |
| |
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 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. |
| |
Keywords: | 6 7-Dimethoxyquinazoline derivative Diaryl urea scaffold Cytotoxic activity |
本文献已被 万方数据 等数据库收录! |
| 点击此处可从《高等学校化学研究》浏览原始摘要信息 |
|
点击此处可从《高等学校化学研究》下载全文 |
|