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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (02): 222-226. 上一篇    下一篇

研究论文

1-取代哌啶-4-酮芳甲酰腙的合成及其抗白血病活性

倪振杰，薛思佳*，王静，孟雯   

  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:2010-07-29 修回日期:2010-09-16 发布日期:2010-11-23
  • 通讯作者: 薛思佳 E-mail:sjxue@sh163.net;sjxue@sohu.com;sjxue@shnu.edu.cn

Synthesis and Anti-leukemia Activity of 1-Substituted Piperidin-4-one Arylformylhydrazones

NI Zhen-Jie, XUE Si-Jia, WANG Jing, MENG Wen   

  1. (College of Life and Environment Science, Shanghai Normal University, Shanghai 200234)
  • Received:2010-07-29 Revised:2010-09-16 Published:2010-11-23

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被引次数

34 | 2

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、酰腙化反应合成了10个未见文献报道的1-取代哌啶-4-酮芳甲酰腙9a～9j, 化合物结构经1H NMR, IR, MS和元素分析确证. 初步的生物活性测试表明, 部分化合物能有效抑制白血病K562细胞的增殖, 具有潜在的抗白血病活性.

关键词: 1-取代哌啶-4-酮, 芳甲酰腙, 合成, 抗白血病活性, K562, MTT

Ten novel 1-substituted piperidin-4-one arylformylhydrazones 9a～9j were synthesized with substituted benzylamines or primary amines as raw materials via a series of Michael addition, Dieckmann condensation, hydrolytic decarboxylation reactions and hydrazone formation reactions. Their structures were elucidated and confirmed by 1H NMR, IR, MS techniques and elemental analysis. The preliminary biologic activity tests indicate that some of the target compounds have good antiproliferative activities against K562 cells and have potential anti-leukemia bioactivity.

Key words: 1-substituted piperidin-4-one, arylformylhydrazone, synthesis, anti-leukemia bioactivity, K562, MTT