Structure-Activity Relationship of Phytoestrogen Analogs as ER alpha/beta Agonists with Neuroprotective Activities
- Authors
- Cho, H.W.; Gim, H.J.; Li, H.; Subedi, L.; Kim, S.Y.; Ryu, J.-H.; Jeon, R.
- Issue Date
- Jan-2021
- Publisher
- Pharmaceutical Society of Japan
- Keywords
- Anti-neuroinflammation; Estrogen receptor agonist; Phytoestrogen; Structure–activity relationship
- Citation
- Chemical and Pharmaceutical Bulletin, v.69, no.1, pp.99 - 105
- Journal Title
- Chemical and Pharmaceutical Bulletin
- Volume
- 69
- Number
- 1
- Start Page
- 99
- End Page
- 105
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/79805
- DOI
- 10.1248/cpb.c20-00706
- ISSN
- 0009-2363
- Abstract
- A set of isoflavononid and flavonoid analogs was prepared and evaluated for estrogen receptor α (ERα) and ERβ transactivation and anti-neuroinflammatory activities. Structure–activity relationship (SAR) study of naturally occurring phytoestrogens, their metabolites, and related isoflavone 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 ERα and ERβ, 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 ERα/β agonists with ERβ selectivity and neuroprotective activity. This study provides knowledge on the SAR of isoflavonoids for further development of potent and selective ER agonists with neuroprotective potential. © 2021 The Pharmaceutical Society of Japan
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