中华医学超声杂志

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N-取代苄基-3,5-双苄叉基-哌啶-4-酮的合成及其抗癌活性的测定

单振国,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:2011-03-28 修回日期:2011-06-13 出版日期:2012-02-10 发布日期:2012-02-10
  • 通讯作者: 薛思佳,教授; Tel/Fax:021-64321926; E-mail:sjxue@sohu.com; 研究方向：精细有机合成与新农药创制
  • 基金资助:
    国家自然科学基金(201042010)和上海市教委重点科技攻关项目(09391212100)资助项目

Synthesis and Anti-tumor activity of N-(Substituted Benzyl) -3,5-bis(Benzylidene)-4-piperidones

SHAN Zhenguo, XUE Sijia*   

  1. (Department of Chemistry,College of Life and Environmental Science,Shanghai Normal University,Shanghai 200234)
  • Received:2011-03-28 Revised:2011-06-13 Published:2012-02-10 Online:2012-02-10

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摘要： 以取代苄胺或伯胺为原料，依次经过Michael加成、Dieckmann缩合、水解脱羧和羟醛缩合反应，合成了10种新化合物(8a～8j)，目标化合物的结构经1H NMR、IR、MS和元素分析确证。 初步的MTT法生物活性测试表明，目标化合物在100 mg/L浓度下能有效抑制白血病K562细胞、乳腺癌HO8910PM细胞和卵巢癌MDR-MB-231细胞的增殖，具有潜在的抗癌活性。

关键词: N-取代哌啶酮, 合成, 抗癌活性, MTT

Abstract: A series of novel N-(substituted benzyl)-3,5-bis(benzylidene)-4-piperidones(8a~8j) were synthesized uisng substituted benzylamines as precursors via a series of Michael addition, Dieckmann condensation, hydrolysis decarboxylation and Aldol condensation. The structures were confirmed by 1H NMR, IR, MS and elemental analysis. The preliminary biological activity tests by MTT assay indicated that some of the target compounds had good antiproliferative activities against K562, MDR-MB-231 and HO8910PM cells, and therefore showed potential anti-tumors bioactivity.

Key words: N-substituted-piperidone, synthesis, antitumor, MTT

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