Synthesis and Screening of Novel Substituted Biphenyl Proteomimetics as Potential Anti-Estrogenic Agents for the Treatment of Hormone-Responsive Breast Cancer
Final rept. 1 Jul 2004-30 Jun 2005
NORTHEASTERN UNIV BOSTON MA
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The goal of this project was to identify one or more novel compounds that would inhibit estrogen receptor coactivator binding proteins. The specific aims involved preparing the requisite aryl halide and boronic acid intermediates, coupling to generate the small biphenyl library and evaluating the compounds in a competitive binding assay. Molecular modeling would be used to help design the compounds and to interpret the results. Molecular modeling suggested that the biphenyl-bis ethers would correctly occupy the target binding site. A series of acidic and basic phenoxy halides were prepared. Conversion to the subsequent aryl boronic acids was less successful and simpler analogs were prepared instead. Model Suzuki couplings were successful and coupling of the aryl halide intermediates with the available aryl boronic acids are in progress. No final compounds are in hand at this time and therefore biological results are unavailable.
- Anatomy and Physiology
- Medicine and Medical Research