四氢吡啶并[4,3-d]二氢嘧啶酮衍生物的合成及其初步抗癌活性测定  

Synthesis and Preliminary Anticancer Activity Evaluation of Tetrahydropyrido[4,3-d]dihydropyrimidine-2-one Derivatives

作　　者：王晶[1] 丁丽[1] 肖笛[1] 薛思佳[1] 

机构地区：[1]上海师范大学生命与环境科学学院化学系,上海200234

出　　处：《有机化学》2012年第11期2187-2192,共6页Chinese Journal of Organic Chemistry

基　　金："十二五"国家科技支撑计划(No.2011BAE06B01-17);国家自然科学基金(Nos.21042010;21102092;30870560)资助项目~~

摘　　要：为寻找新型抗癌药物的先导化合物,设计合成了16种未见文献报道的四氢吡啶并[4,3-d]二氢嘧啶酮衍生物2a～2p,结构经1H NMR,IR,MS,元素分析确证.初步的生物活性测试结果表明,在100μg/mL浓度下,目标化合物对白血病K562细胞的增殖表现出显著的抑制活性,对卵巢癌HO-8910和肝癌SMMC-7721细胞系的增殖也表现出一定的抑制活性.In search of more effective anticancer agents, sixteen novel tetrahydropyrido[4,3-d]dihydropyrimidine-2-one derivatives 2a-2p were synthesized by reacting N-O-substituted benzyl）-3,5-bisbenzylidene-4-piperidone with urea in EtONa/EtOH under reflux condition. The structures were confirmed by 1H NMR, IR, MS and elemental analysis. The preliminary bioassay indicated that some title compounds exhibited good antiproliferative activities against K562 cells, certain antiproliferative activities against ovarian cancer HO-8910 cells and liver cancer SMMC-7721 cells.

关 键 词：四氢吡啶并[4 3-d]二氢嘧啶酮 衍生物 合成 白血病K562 抗癌活性 

分 类 号：TQ463.5[化学工程—制药化工]