Daucane phytoestrogens: A structure-activity study
Daucane phytoestrogens: A structure-activity study
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DOI：
10.1021/np0201671
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发表时间：
2002-11-01
影响因子：
5.1
通讯作者：
Milligan, S
中科院分区：
文献类型：
--
作者：
Appendino, G;Spagliardi, P;Milligan, S
在含有人雌激素受体α的酵母筛选中，研究了一系列酰基修饰的胡萝卜烷酯ferutinin（1a）类似物的雌激素活性。观察到相当严格的结构-活性关系。因此，虽然母体polvol（jaeschkeanadiol，2a）无活性，但对羟基苯甲酰基部分的存在对于酵母筛选中的活性是必需的。同源化和乙烯基化都对活性有害，对羟基取代基的甲基化和相邻碳上氧官能团的引入也是如此。
The estrogenic activity of a series of analogues of the daucane ester ferutinin (1a) modified at the acyl moiety was investigated in a yeast screen containing the human estrogen receptor a. Rather strict structure-activity relationships were observed. Thus, while the parent polvol (jaeschkeanadiol, 2a) was inactive, the presence of a p-hydroxybenzoyl moiety was necessary for activity in the yeast screen. Homologation and vinylation were both detrimental for activity, as were methylation of the p-hydroxyl substituent and the introduction of oxygen functions on the adjacent carbons.