【摘要】 以金雀异黄素为母体,取代氨基烷氧基为侧链,设计、合成了20个金雀异黄素衍生物,其中16个未见文献报道,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,以研究其潜在的雌激素受体调节活性。结果表明,化合物4a、4b、4d、4e及4f对MCF-7细胞的增殖有显著的抑制作用,48 h和72 h的抑制率均大于40%(P<0.01)。化合物8d及9a对MCF-7细胞增殖具有一定的促进作用;化合物9d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15%(P<0.05)。更多还原

【Abstract】 Twenty genistein derivatives with various basic side chains were synthesized and their structures were confirmed by IR,ESI-MS and 1H 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).更多还原