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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (11): 1852-1863. 上一篇    下一篇

研究论文

具有选择性雌激素受体调节活性的大豆苷元衍生物的合成及生物活性研究

芦金荣，桂力，沙磊，江振洲，张娟，周丽丽，黄文龙*   

  1. (1中国药科大学有机化学教研室 南京 210009)
    (2中国药科大学新药研究中心 南京 210009)
    (3中国药科大学新药筛选中心 南京 210009)
  • 收稿日期:2011-02-19 修回日期:2011-05-28 发布日期:2011-06-21
  • 通讯作者: 芦金荣 E-mail:L_John638185@yahoo.com.cn

Synthesis, Characterization of a Series of Daidzein Derivatives as Selective Estrogen Receptor Modulator

LU Jin-Rong, GUI Li, SHA Lei, JIANG Zhen-Zhou, ZHANG Juan, ZHOU Li-Li, HUANG Wen-Long   

  1. (1 Department of Organic Chemistry, China Pharmaceutical University, Nanjing 210009)
    (2 Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009)
    (3 New Drug Screening Center, China Pharmaceutical University, Nanjing 210009)
  • Received:2011-02-19 Revised:2011-05-28 Published:2011-06-21

PDF

1027

被引次数

6

以大豆苷元为母体, 取代氨基烷氧基为侧链, 设计、合成了28个结构新颖的未见文献报道的大豆苷元衍生物, 并检测了其对雌激素受体阳性的人乳腺癌细胞株MCF-7的体外活性. 结果表明, 化合物4c, 4g及6a对MCF-7的增殖有显著的抑制作用, 48, 72 h的抑制率均大于50% (p＜0.01). 化合物11h具有显著的促进MCF-7细胞增殖的作用, 48, 72 h的增殖率均大于20% (p＜0.05)|化合物10a作用48 h时对MCF-7细胞的增殖有显著的促进作用, 增殖率大于10% (p＜0.05).

关键词: 异黄酮, 大豆苷元, 选择性雌激素受体调节剂, MCF-7细胞增殖, 合成

Twenty eight novel daidzein derivatives with various basic side chains structure were synthesized and their bioactivity to estrogen receptor (ER) level of human breast cancer MCF-7 cells was evaluated in vitro. The results indicated that compounds 4c, 4g and 6a showed quite potent inhibition on MCF-7 cells proliferation with more than 50% of inhibitive rates at 48 and 72 h (p＜0.01). Compound 11h could significantly induce MCF-7 cells proliferation with more than 20% of growth rates at 48 and 72 h (p＜0.05), and compound 10a with more than 10% of growth rate showed the similar activity at 48 h (p＜0.05).

Key words: isoflavones, daidzein, selective estrogen receptor modulator (SERM), MCF-7 cells proliferation, synthesis