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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (9): 1445-1449. 上一篇    下一篇

研究简报

8-黄酮哌嗪衍生物的合成及生理活性研究

郑梅花a 甘 莹b 谢松强b 王超杰a,b 赵 瑾*,a,b   

  1. (a河南大学化学化工学院 开封 475004)
    (b河南大学天然药物与免疫工程重点实验室 开封 475004)
  • 收稿日期:2008-12-31 修回日期:2009-04-24 发布日期:2009-12-30
  • 通讯作者: 赵 瑾

Synthesis and Biological Activity of 8-Piperazinomethylflavone Derivatives

Zheng, Meihua a Gan, Ying b Xie, Songqiang b Wang, Chaojie a,b Zhao, Jin *,a,b   

  1. (a College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475004)
    (b Key Laboratory of Natural Medicine and Immune Engineering, Henan University, Kaifeng 475004)
  • Received:2008-12-31 Revised:2009-04-24 Published:2009-12-30
  • Contact: Zhao, Jin

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被引次数

12 | 3

设计合成了4个8-黄酮甲基哌嗪和4个8-黄酮甲基多聚异戊二烯哌嗪类化合物, 产物结构均经1H NMR, ESI-MS和元素分析确认. 使用MTT法测试了8个化合物对Bel-7402 (人肝癌细胞)和K562(白血病细胞)两种肿瘤细胞的体外抗肿瘤活性. 结果表明哌嗪单黄酮和双黄酮体外生理活性并不理想, 但在黄酮骨架上引入多聚异戊二烯哌嗪基后的产物对K562细胞表现出比N,N-二(8-黄酮甲基)香叶基胺(1)更好的体外抗肿瘤活性.

关键词: 黄酮衍生物, 合成, 生理活性

Four 8-piperazinomethylflavone and four 8-flavonemethyl-polyisoprenylpiperazine derivatives were designed, synthesized, and structurally were confirmed by 1H NMR, ESI-MS techniques and elemental analysis. The prelimilary antitumor activity was evaluated on Bel-7402 and K562 cell lines by MTT assay. The results demonstrated that 8-flavonemethyl-piperazines and N,N-di(8-flavonemethyl)piperazines did not exhibit antitumor activity. However, two N-(8-flavonemethyl)-N’-polyisoprenylpiperazines possessed better antitumor activity against K562 cell lines than prior N,N-bis(8-flavonemethyl)geranylamine (1).

Key words: synthesis, biological activity, flavone derivative