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Description
Title: | Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors |
Author(s): | Collins, Margaret Lynn |
Doctoral Committee Chair(s): | Katzenellenbogen, John A. |
Department / Program: | Chemistry |
Discipline: | Chemistry |
Degree Granting Institution: | University of Illinois at Urbana-Champaign |
Degree: | Ph.D. |
Genre: | Dissertation |
Subject(s): | Health Sciences, Oncology |
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. |
Issue Date: | 2004 |
Type: | Text |
Language: | English |
Description: | 120 p. Thesis (Ph.D.)--University of Illinois at Urbana-Champaign, 2004. |
URI: | http://hdl.handle.net/2142/84147 |
Other Identifier(s): | (MiAaPQ)AAI3153275 |
Date Available in IDEALS: | 2015-09-25 |
Date Deposited: | 2004 |
This item appears in the following Collection(s)
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Dissertations and Theses - Chemistry
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Graduate Dissertations and Theses at Illinois
Graduate Theses and Dissertations at Illinois