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

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. (c) 2005 Elsevier Ltd. All rights reserved.