ScholarWorks@숙명여자대학교

초록

A set of isollavononid and llavonoid analogs was prepared and evaluated for estrogen receptor alpha (ER alpha) and ER beta transactivation and anti-neuroinflammatory activities. Structure activity relationship (SAR) study of naturally occurring phytoestrogens, their metabolites, and related isollavone analogs revealed the importance of the C-ring of isoflavonoids for ER activity and selectivity. Docking study suggested putative binding modes of daidzein 2 and dehydroequol 8 in the active site of ER alpha and ER beta, and provided an understanding of the promising activity and selectivity of dehydroequol 8. Among the tested compounds, equol 7 and dehydroequol 8 were the most potent ER alpha/beta agonists with ER beta selectivity and neuroprotective activity. This study provides knowledge on the SAR of isollavonoids for further development of potent and selective ER agonists with neuroprotective potential.

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