Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives

A diastereomerically pure series of 7α-thioestratrienes was prepared and evaluated for its affinity for both the human estrogen receptor α and the more recently discovered estrogen receptor β. The functional estrogenic activities of the compounds were measured in a MCF-7 ERE-tk-luciferase assay. The activities and selectivities of the compounds were sensitive to the nature of the thioether side chain.