Author/Authors :
Timothy I. Richardson، نويسنده , , Bryan H. Norman، نويسنده , , Charles W. Lugar III، نويسنده , , Scott A. Jones، نويسنده , , Yong Wang، نويسنده , , Jim D. Durbin، نويسنده , , Venkatesh Krishnan، نويسنده , , Jeffrey A. Dodge، نويسنده ,
Abstract :
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.
