- 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.
Bioorganic & medicinal chemistry letters (2005-02-17)
Lawrence G Hamann, J Hoyt Meyer, Daniel A Ruppar, Keith B Marschke, Francisco J Lopez, Elizabeth A Allegretto, Donald S Karanewsky
PMID15713407
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.