Synthesis and Biological Evaluation of Coactivator Binding Inhibitors and Bivalent Ligands for the Estrogen Receptor

Synthesis and Biological Evaluation of Coactivator Binding Inhibitors and Bivalent Ligands for the Estrogen Receptor

137 pages· 2008· ISBN 9780549909576
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The synthesis of steroidal bivalent ligands for ER is also reported. Two estradiol molecules were connected through a phenylethynyl linkage with chemical tethers of varying composition and length. The binding properties of the bivalent ligands for ER were measured. Moderate relative binding affinities were obtained and in some cases biphasic binding curves were observed.

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