Physicochemical Characterization of -hydroxyphenyl Phosphine Borane Derivatives and Their Evaluation As Nuclear Estrogen Receptor Ligands

Overview

Journal RSC Med Chem

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2024 Jan 29

PMID 38283218

Authors

Yu Miyajima

Tomomi Noguchi-Yachide

Kotaro Ochiai

Shinya Fujii

Affiliations

Soon will be listed here.

Abstract

Increasing the structural options in medicinal chemistry is a promising approach to develop new drug candidates. In this research, we designed and synthesized a series of -hydroxyphenyl phosphine borane derivatives and investigated their structure-property and structure-activity relationships. The synthesized -phenylphosphine borane derivatives exhibited sufficient stability in aqueous media, weaker hydrophobicity than the corresponding alkanes and silanes, and sufficient affinity for lipid membranes to enable permeability. Several -hydroxyphenyl phosphine borane derivatives exhibited significant estrogen receptor (ER) agonistic activity with superior ligand-lipophilicity efficiency (LLE). The phosphine borane framework appears to be a promising option for structural development in drug discovery studies.

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