含嘧啶氨基的三取代三嗪衍生物的合成及其抗菌、抗肿瘤活性研究  

Synthesis and Antifungal,Anti-tumor Studies of the Trisubstitued Triazines Bearing Aminopyrimidine Group

作　　者：陈华[1] 谷云景[1] 苑香果[1] 赵莲[1] 赵建鹏[1] 秦占斌[1] 刘丽[2] 李小六[1] 曹克强[2] 张金超[1] 

机构地区：[1]河北大学化学与环境科学学院河北省化学生物学重点实验室保定0710021 [2]河北农业大学植物保护学院保定071001

出　　处：《有机化学》2011年第8期1266-1271,共6页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.20902016);河北省科学技术研究与发展计划(No.09276418D-13)资助项目

摘　　要：以三聚氯氰为起始原料,合成了系列新的含嘧啶氨基的2,4,6-三取代-1,3,5-三嗪化合物,并测试了化合物抗苹果树腐烂病菌和抑制肿瘤细胞增殖活性.结果表明,化合物2aa～2cb及3aa～3cb对苹果树腐烂病菌具有显著的抑制作用,具有开发为新型植物抗菌剂的潜力.部分化合物,如4ba和4ca分别对胃癌(BGC-823)和宫颈癌(Hela)肿瘤细胞具有较强的抑制活性,IC50分别为10.9和11.3μmol/L.A series of novel trisubstituted 1,3,5-triazine compounds bearing aminopyrimidine group were synthesized using cyanuric chloride as the starting material. The antifungal activitiy against Valsa mall and antiproliferative activity for three tumor cells of all the triazine compounds were evaluated. The results showed that a majority of the compounds 2aa^2cb and 3aa^3cb have notable inhibitory activity against Valsa mall Some compounds, such as 4ba and 4ca, showed good cytotoxicity to BGC-823 and Hela tumor cells with the IC50 value of 10.9 and 11.3 ~tmol/L, respectively, higher than that of the positive control cis- platin.

关 键 词：嘧啶氨基 三嗪化合物 抗菌活性 抗肿瘤活性 

分 类 号：R96[医药卫生—药理学] TQ460.1[医药卫生—药学]