Synthesis and Biochemical Characterization of a Series of 17α-Perfluoroalkylated Estradiols as Selective Ligands for Estrogen Receptor α

Abstract

17α-perfluoroalkylated estradiols were synthesized by Ru-catalyzed cross metathesis reactions of 17α-allyl- or 17α-vinylestradiols with perfluoroalkylpropenes. Compounds were tested in both agonistic and antagonistic modes using a panel of stable steroid receptor reporter cell lines.

Keywords

• 17α-perfluoroalkylated estradiols
• selective ligands
• estrogen receptors