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Estrogenic antagonists bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore
1Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan.
Bioorganic & Medicinal Chemistry Letters
|January 5, 2000
Abstract:
Dicarba-closo-dodecaboranes (carboranes), which have spherical geometry and hydrophobicity, are applicable as a hydrophobic pharmacophore of biologically active molecules. We have designed and synthesized estrogenic antagonists based on the structure of the potent agonist 1-hydroxymethyl-12-(4-hydroxyphenyl)-1,12-dicarba-closo-d odecaborane, which we have developed. The compounds showed potent antagonistic activity in luciferase reporter gene assay using COS-1 cells transfected with rat ER alpha-expression plasmid and an appropriate reporter plasmid.