Synthesis and biological evaluation of novel 6-chloro-quinazolin derivatives as potential antitumor agents
文献类型： 外文期刊
作者： Luo, Hui 1 ; Yang, Shengjie 2 ; Cai, Yongqiang 1 ; Peng, Zhijun 1 ; Liu, Tao 1 ;
作者机构： 1.Guizhou Acad Agr Sci, Guizhou Fruit Inst, Guiyang 550006, Peoples R China
2.Yangtze River Pharmaceut Grp Co Ltd, Res Inst Tradit Chinese Med, Taizhou 225321, Peoples R China
3.Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang 550025, Peoples R China
关键词： Synthesis;6-Chloro-quinazolin derivatives;Antitumor;Cancer cells;Apoptosis
期刊名称：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：6.514； 五年影响因子：6.099 ）
ISSN： 0223-5234
年卷期： 2014 年 84 卷
页码：
收录情况： SCI
摘要： Series of novel derivatives of 6-chloro-quinazolin, which this moiety was linked to a 1,5-diaryl-1,4-pentadien-3-one system, have been synthesized and tested for their antitumor activities in vitro against a panel of three human cancer cell lines (MGC-803, Bcap-37, and PD cells). Bioassay results indicated that most of the prepared compounds demonstrated good activities against various cancer cells. 6-chloro-quinazolin derivatives 5a and 5f were the most active members in this study, and experimental results of fluorescent staining and flow cytometry analysis revealed that they could induce apoptosis in MGC-803 and Bcap-37 cells, with apoptosis ratios of 31.7% and 21.9% at 24 h of treatment at 10 mu M in MGC-803 cells. Those two quinazoline derivatives could be considered as useful templates for future development to obtain more potent antitumor agents. (C) 2014 Elsevier Masson SAS. All rights reserved.
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