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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
【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.
【Abstract】 In search of more effective anticancer agents,sixteen novel tetrahydropyrido[4,3-d]dihydropyrimidine-2-one derivatives 2a ～ 2p were synthesized by reacting N-(4-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.
【Key words】 tetrahydropyrido[4,3-d]dihydropyrimidine-2-one； derivative； synthesis； leukemic K562 cells； anticancer activities；
- 【文献出处】 有机化学 ,Chinese Journal of Organic Chemistry , 编辑部邮箱 ,2012年11期
- 【分类号】TQ463.5
- 【被引频次】3
- 【下载频次】276