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Structure-Activity Relationship of Phytoestrogen Analogs as ER alpha/beta Agonists with Neuroprotective Activities

Authors
Cho, Hye WonGim, Hyo JinLi, HuaSubedi, LalitaKim, Sun YeouRyu, Jae-HaJeon, Raok
Issue Date
Jan-2021
Publisher
PHARMACEUTICAL SOC JAPAN
Keywords
phytoestrogen; estrogen receptor agonist; structure activity relationship; anti-neuroinflmmation
Citation
CHEMICAL & PHARMACEUTICAL BULLETIN, v.69, no.1, pp 99 - 105
Pages
7
Journal Title
CHEMICAL & PHARMACEUTICAL BULLETIN
Volume
69
Number
1
Start Page
99
End Page
105
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/146838
DOI
10.1248/cpb.c20-00706
ISSN
0009-2363
1347-5223
Abstract
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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