2. Academic Validation
  3. Androstene-3,5-dienes as ER-beta selective SERMs

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

Affiliation

  • 1 Merck Research Laboratories, Rahway, NJ 07065, USA. tim_blizzard@merck.com
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).

Figures