Daucane phytoestrogens: A structure-activity study

被引：64
作者：
Appendino, G
Spagliardi, P
Cravotto, G
Pocock, V
Milligan, S
机构：
[1] Univ Piemonte Orientale, Dipartimento Sci Chim Alimentari Farmaceut & Farm, I-28100 Novara, Italy
[2] Dipartimento Sci & Tecnol Farmaco, I-10125 Turin, Italy
[3] Endocrinol & Reprod Res Grp, London SE1 1UL, England
来源：
JOURNAL OF NATURAL PRODUCTS | 2002年 / 65卷 / 11期
关键词：
D O I：
10.1021/np0201671
中图分类号：
Q94 [植物学];
学科分类号：
071001 ;
摘要：
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.
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页码：1612 / 1615
页数：4
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