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有机化学
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有机化学 ›› 2008, Vol. 28 ›› Issue (01): 84-88. 上一篇    下一篇

研究论文

8-取代黄酮的合成及生理活性研究

赵瑾a，刘洋a，郑梅花a，谢松强b，王超杰*,a,c   

  1. (a河南大学化学化工学院 开封 475001)
    (b河南大学药学院 开封 475001)
    (c河南大学天然产物与药物化学研究所 开封 475001)
  • 收稿日期:2006-12-28 修回日期:1900-01-01 发布日期:2008-01-23
  • 通讯作者: 王超杰

Synthesis and Biological Activity of 8-Substituted Flavonoids

ZHAO Jina, LIU Yanga, ZHENG Mei-Huaa, XIE Song-Qiangb, WANG Chao-Jie*,a,c   

  1. (a College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475001)
    (b College of Pharmacy, Henan University, Kaifeng 475001)
    (c Institute of Natural Products & Medicinal Chemistry, Henan University, Kaifeng 475001)
  • Received:2006-12-28 Revised:1900-01-01 Published:2008-01-23
  • Contact: WANG Chao-Jie

PDF

941

被引次数

21

设计合成了8-黄酮甲基氮芥和6种8-黄酮甲基多聚异戊二烯胺类化合物, 产物结构经1H NMR, MS及元素分析确证. 合成的7个化合物与氮芥类抗肿瘤药物美法仑一起对白血病细胞(K562)、中国仓鼠卵巢细胞(CHO)、黑色素瘤细胞(B16)等3种肿瘤细胞进行了初步的体外生理活性测试. 结果表明, 对3种受测细胞, 8-黄酮甲基氮芥的体外活性均与美法仑接近; N,N-二(8-黄酮甲基)香叶基胺则表现出比美法仑更高的体外抗肿瘤活性.

关键词: 黄酮, 合成, 生理活性

One 8-flavonemethyl nitrogen mustard and six 8-flavonemethyl-polyisoprenylamines were designed and synthesized. The structures of the target compounds were confirmed by 1H NMR, mass spectra and elemental analysis. All compounds, together with the commercial drug melphalan, were tested in vitro for their inhibition on three kinds of cancer cells, K562, CHO and B16. The results demonstrated that the activity of 8-flavonemethyl nitrogen mustard was similar to that of melphalan, while N,N-bis(8-flavone- methyl)geranylamine possessed higher antitumor activity than melphalan.

Key words: synthesis, flavone, biological activity