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Physicochemical characterization of B-hydroxyphenyl phosphine borane derivatives and their evaluation as nuclear
Yu Miyajima1, Tomomi Noguchi-Yachide2, Kotaro Ochiai1
1Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University 2-3-10 Kanda-Surugadai Chiyoda-ku Tokyo 101-0062 Japan fujiis.chem@tmd.ac.jp.
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 B-hydroxyphenyl phosphine borane derivatives and investigated their structure-property and structure-activity relationships. The synthesized B-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 B-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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