Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (10): 2725-2735.DOI: 10.6023/cjoc201705013 Previous Articles     Next Articles



宋攀攀a,b, 栗娜a,b, 崔飞a,b, 辛景超a,b, 张孝松a,b, 曹钦坡a,b, 王超杰a,b, 戴文杰a, 孟祥川a, 刘梦a, 常通航a, 柳晴怡a, 孙月红a, 可钰a,b, 张秋荣a,b, 刘宏民a,b   

  1. a 郑州大学药学院 郑州 450001;
    b 新药创制与药物安全性评价河南省协同创新中心 郑州 450001
  • 收稿日期:2017-05-08 修回日期:2017-05-23 发布日期:2017-06-07
  • 通讯作者: 可钰, 张秋荣, 刘宏民;;
  • 基金资助:


Synthesis and Antitumor Activity Evaluation of 2,4,6-Trisubstituted Pyrimidine Derivatives

Song Panpana,b, Li Naa,b, Cui Feia,b, Xin Jingchaoa,b, Zhang Xiaosonga,b, Cao Qinpoa,b, Wang Chaojiea,b, Dai Wenjiea, Meng Xiangchuana, Liu Menga, Chang Tonghanga, Liu Qingyia, Sun Yuehongaa, Ke Yua,b, Zhang Qiuronga,b, Liu Hongmina,b   

  1. a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
    b Collaborative Innovation Center of New Drug Research and Saftry Evaluation, Zhengzhou 450001
  • Received:2017-05-08 Revised:2017-05-23 Published:2017-06-07
  • Contact: 10.6023/cjoc201705013;;
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.81430085) and the Research Project of Science and Technology Bureau of Zhengzhou City (No.141PQYJS554).

With the aim of obtaining potential antitumor candidates with more efficiency and more economic value. 40 2,4,6-trisubstituted pyrimidine derivatives bearing chalcone moiety were synthesized via cyclization, chlorination, substitution with benzoylacetate and ethylacetoacetate as the starting materials. The structures of target products were confirmed by 1H NMR, I3C NMR and HRMS. 2,4,6-Trisubstituted pyrimidine derivatives bearing chalcone moiety were evaluated for anticancer activity on four human cancer cell lines including EC-109, MGC-803, HepG-2 and MDA-MB-231 by CCK-8 (cell counting Kit-8) assay. Among them, (E)-1-(4-((2-(((1H-benzo[d]imidazol-2-yl)methyl)thio)-6-methylpyrimidin-4-yl)amino)-phe-nyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (13u) were more cytotoxic against MGC-803 and MDA-MB-231 cell lines, with IC50 values of 0.99 and 1.77 μmol·L-1, respectively.

Key words: 2,4,6-trisubstituted pyrimidine, chalcone, antitumor