Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors
Collins, Margaret Lynn
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https://hdl.handle.net/2142/84147
Description
Title
Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors
Author(s)
Collins, Margaret Lynn
Issue Date
2004
Doctoral Committee Chair(s)
Katzenellenbogen, John A.
Department of Study
Chemistry
Discipline
Chemistry
Degree Granting Institution
University of Illinois at Urbana-Champaign
Degree Name
Ph.D.
Degree Level
Dissertation
Keyword(s)
Health Sciences, Oncology
Language
eng
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. 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.
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