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Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives
C P Miller1, I Jirkovsky, B D Tran
1Chemical Sciences, Wyeth-Ayerst Research, Radnor, PA 19087, USA.
Abstract:
A diastereomerically pure series of 7alpha-thioestratrienes was prepared and evaluated for its affinity for both the human estrogen receptor alpha and the more recently discovered estrogen receptor beta. 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.
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