Androstene-3,5-dienes as ER-beta selective SERMs

  • Bioorg Med Chem Lett. 2007 Nov 15;17(22):6295-8. doi: 10.1016/j.bmcl.2007.09.001.
Timothy A Blizzard  1 ,  Candido Gude ,  Jerry D Morgan 2nd ,  Wanda Chan ,  Elizabeth T Birzin ,  Marina Mojena ,  Consuelo Tudela ,  Fang Chen ,  Kristin Knecht ,  Qin Su ,  Bryan Kraker ,  Ralph T Mosley ,  Mark A Holmes ,  Susan P Rohrer ,  Milton L Hammond
Affiliations
PMID: 17890084 DOI: 10.1016/j.bmcl.2007.09.001
Abstract

A series of androstene-3,5-diene derivatives were prepared. Despite lacking the C-3 hydroxyl previously believed necessary for ER activity, some of the analogs retained surprising affinity for ER-beta. For example, diene 4 retained excellent selectivity and potency as an ER-beta agonist and was more selective for ER-beta over the Androgen Receptor (AR).