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有机化学
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有机化学 ›› 2012, Vol. 32 ›› Issue (11): 2187-2192.DOI: 10.6023/cjoc201206006 上一篇    下一篇

研究简报

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

王晶, 丁丽, 肖笛, 薛思佳   

  1. 上海师范大学生命与环境科学学院化学系 上海 200234
  • 收稿日期:2012-06-06 修回日期:2012-06-27 发布日期:2012-07-04
  • 通讯作者: 薛思佳 E-mail:sjxue@shnu.edu.cn
  • 基金资助:

    “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.

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

Wang Jing, Ding Li, Xiao Di, Xue Sijia   

  1. College of Life and Environment Sciences, Shanghai Normal University, Shanghai 200234
  • Received:2012-06-06 Revised:2012-06-27 Published:2012-07-04
  • Supported by:

    Project supported by the Key Scientific “Twelfth Five-Year” National Technology Support Program (No. 2011BAE06B01-17), and the National Natural Science Foundation of China (Nos. 21042010, 21102092, 30870560).

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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100 μg/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.

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

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