Estrogenic antagonists bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore.
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.
Endo
Y
Y
Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan.
Yoshimi
T
T
Iijima
T
T
Yamakoshi
Y
Y
D000818:Animals; D001896:Boron Compounds / Q000737:chemistry*; D019556:COS Cells; D004965:Estrogen Antagonists / Q000737:chemistry* / Q000494:pharmacology; D017930:Genes, Reporter; D008156:Luciferases / Q000235:genetics; D008958:Models, Molecular; D051381:Rats
D001896:Boron Compounds; D004965:Estrogen Antagonists; D008156:Luciferases