Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold

  • Bioorg Med Chem Lett. 2005 Mar 1;15(5):1463-6. doi: 10.1016/j.bmcl.2004.12.077.
Lawrence G Hamann  1 ,  J Hoyt Meyer ,  Daniel A Ruppar ,  Keith B Marschke ,  Francisco J Lopez ,  Elizabeth A Allegretto ,  Donald S Karanewsky
Affiliations
  • 1. Department of Medicinal Chemistry, Ligand Pharmaceuticals, 10275 Science Centre Dr., San Diego, CA 92121, USA. [email protected]
PMID: 15713407 DOI: 10.1016/j.bmcl.2004.12.077
Abstract

An oxabicyclic template for Estrogen receptor alpha and beta agonists has been identified which can be tuned to provide moderate levels of selectivity for either receptor sub-type. Structure-activity relationships within this phenol-substituted oxabicyclo[3.3.1]nonene series are described. Select compounds from the present series showed activity in vivo after oral dosing in rodent models of uterine proliferation.