In practice, antagonistic xenoestrogen compounds have been used as drugs to treat cancer. Traditional strategies, include preparation of estrogen receptor antagonists exhibiting high affinity for the receptor while preventing rearrangement of the AF-2 binding domain. In a potentially new strategy, substituted parabens have proven to act as antagonists but do not bear the large sidechain associated with this common antagonist strategy. Weak phenolic interactions make determining such paraben binding confirmations and mode of action difficult. To investigate these activities associated with hindered phenolic compounds, substituted bisphenol probes have been synthesized <i>via </i>Witting protocols to produce a series of stilbene derivatives. Herein we present the synthesis of such substituted stilbenes. The binding energies of this library will be determined by TR-FRET and efficacies determined by ELISA. Antagonism is expected to arise from similar disruption in the role of H12 in the AF-2 ligand binding domain albeit due to alternative binding interactions.

Synthesis of substituted bisphenol probes towards the investigation of antagonistic effects observed with 3,5-substituted paraben derivatives

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.