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

Abstract An oxabicyclic template for estrogen receptor α and β 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.