Benzopyrans as selective estrogen receptor β agonists (SERBAs). Part 2: Structure–activity relationship studies on the benzopyran scaffold

Benzopyrans are selective estrogen receptor (ER) β agonists (SERBAs), which bind the ER subtypes α and β in opposite orientations. Here we describe structure–activity relationship studies that led to the discovery of bezopyran 5b. X-ray crystal structures of 5b and a non-selective analog 5c in ERα help explain the observed selectivity of the benzopyran platform.

Structure–activity relationship studies that lead to the discovery of benzopyran 5b are reported.Figure optionsDownload as PowerPoint slide