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| 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 | |
| 引用本文： | 芦金荣,桂力,沙磊,江振洲,张娟,周丽丽,黄文龙.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[J].有机化学,2011,31(11). |
| 作者姓名： | 芦金荣 桂力 沙磊 江振洲 张娟 周丽丽 黄文龙 |
| 作者单位： | 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 |
| 摘 要： | 以大豆苷元为母体,取代氨基烷氧基为侧链,设计、合成了28个结构耨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,48,72h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 |
Synthesis, Characterization of a Series of Daidzein Derivatives as Selective Estrogen Receptor Modulator |
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| Lu, Jinrong,Gui, Li,Sha, Lei,Jiang, Zhenzhou,Zhang, Juan,Zhou, Lili,Huang, Wenlong.Synthesis, Characterization of a Series of Daidzein Derivatives as Selective Estrogen Receptor Modulator[J].Chinese Journal of Organic Chemistry,2011,31(11). | |
| Authors: | Lu Jinrong Gui Li Sha Lei Jiang Zhenzhou Zhang Juan Zhou Lili Huang Wenlong |
| Institution: | Lu,Jinronga Gui,Lib Sha,Leib Jiang,Zhenzhouc Zhang,Juanc Zhou,Lilia Huang,Wenlong b(a Department of Organic Chemistry,China Pharmaceutical University,Nanjing 210009)(b Center of Drug Discovery,Nanjing 210009)(c New Drug Screening Center,Nanjing 210009) |
| Abstract: | Twenty eight novel daidzein derivatives with various basic side chains structure were synthe-sized 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 signifi-cantly induce MCF-7 cells proliferation with more than 20% of growth rates at 48 and 72 h(p<0.05),and c... |
| Keywords: | isoflavones daidzein selective estrogen receptor modulator(SERM) MCF-7 cells prolifera-tion synthesis |
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