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

…, JH Meyer, DA Ruppar, KB Marschke, FJ Lopez…

Index: Hamann, Lawrence G.; Meyer, J. Hoyt; Ruppar, Daniel A.; Marschke, Keith B.; Lopez, Francisco J.; Allegretto, Elizabeth A.; Karanewsky, Donald S. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 5 p. 1463 - 1466

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Citation Number: 22

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.