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LU Jin-rong, HUANG Wen-long, JIANG Zhen-zhou, ZHANG Juan, ZHANG Zhao-qi, ZHU Ping. Synthesis and characterization of a series of genistein derivatives as selective estrogen receptor modulators[J]. Journal of China Pharmaceutical University, 2011, 42(6): 495-502.
Citation: LU Jin-rong, HUANG Wen-long, JIANG Zhen-zhou, ZHANG Juan, ZHANG Zhao-qi, ZHU Ping. Synthesis and characterization of a series of genistein derivatives as selective estrogen receptor modulators[J]. Journal of China Pharmaceutical University, 2011, 42(6): 495-502.

Synthesis and characterization of a series of genistein derivatives as selective estrogen receptor modulators

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  • Twenty genistein derivatives with various basic side chains were synthesized and their structures were confirmed by IR,ESI-MS and 1H NMR.Among these compounds,sixteen compounds have not been reported in the literatures.The effect of the target compounds on estrogen receptor levels of human breast cancer MCF-7 cells was evaluated in vitro in order to study the potency in selective modulation of estrogen receptor.The results indicated that compounds 4a , 4b , 4d , 4e and 4f showed quite potent inhibition on MCF-7 cells proliferation with inhibitive rates of more than 40% at 48 h and 72 h (P<0.01).Compound 9d could significantly induce MCF-7 cells proliferation with a growth rate of more than 15% at 48 h (P<0.05).
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