Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors

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.

Name thesis:degree_name

Ph.D.

Level thesis:degree_level

Dissertation

Discipline thesis:degree_discipline

Chemistry

Grantor

University of Illinois at Urbana-Champaign

Year dc:date

2015

Author dc:creator

• Collins, Margaret Lynn

Contributors dc:contributor

• Katzenellenbogen, John A.

• Health Sciences, Oncology

Language dc:language

eng

Identifier

(MiAaPQ)AAI3153275

OAI identifier oai:identifier

oai:www.ideals.illinois.edu:2142/84147