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Updated: Jul 16, 2025

Imine Metathesis by Silica-Supported Catalysts Using the Methodology of Surface Organometallic Chemistry
Published on: October 18, 2019
Development of subtype-selective estrogen receptor modulators using the bis(4-hydroxyphenyl)silanol core as a stable
Yuichiro Matsumoto1, Yuichi Hashimoto1, Shinya Fujii2
1Institute for Quantitative Biosciences, The University of Tokyo 1-1-1 Yayoi, Bunkyo-ku Tokyo 113-0032 Japan.
Abstract:
In this study, we synthesized and evaluated silanol-based bisphenol derivatives as stable isosteres of bis(4-hydroxyphenyl)methanol. The developed silanols exhibited estrogen receptor (ER)-modulating activity. Among them, bis(4-hydroxyphenyl)(methyl)silanol (5a) showed a characteristic ER subtype selectivity, namely, antagonistic activity toward ERα and agonistic activity toward ERβ. Docking simulation indicated that the silanol moiety plays a key role in this selectivity. Our results suggest that silanol-based bisphenols offer a unique scaffold for biologically active compounds.
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