{"id":{"repo_id":"uiuc","oai_identifier":"oai:www.ideals.illinois.edu:2142/84147"},"canonical_url":"https://search.dev.ndltd.org/etd/uiuc/oai:www.ideals.illinois.edu:2142/84147","repository":{"repo_id":"uiuc","name":"University of Illinois - Urbana-Champaign","base_url":"https://www.ideals.illinois.edu/oai-pmh"},"display":{"title":"Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors","abstract":"Key hydrophobic and hydrogen bonding moieties were incorporated onto a variety of core scaffolds including amphipathic benzene, bicyclo[2.2.2]octane, and urea, resulting in three different series of compounds that could be utilized as coactivator binding inhibitors (CBIs). A fluorescence-based assay was used to evaluate the ability of the CBIs to effectively block the ER-coactivator interaction. 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A fluorescence-based assay was used to evaluate the ability of the CBIs to effectively block the ER-coactivator interaction. The most effective compounds synthesized were amphipathic benzene derivatives with Ki's of 7 and 4 muM, which are the best in vitro affinities to date in our research group.","Made available in DSpace on 2015-09-25T22:13:11Z (GMT). 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