2. Academic Validation
  3. Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold

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

Affiliation

  • 1 Department of Medicinal Chemistry, Ligand Pharmaceuticals, 10275 Science Centre Dr., San Diego, CA 92121, USA. lawrence.hamann@bms.com
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.

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