Synthesis of Biphenyl Proteomimetics as Estrogen Receptor-α Coactivator Binding Inhibitors

A novel series of biphenyl proteomimetic compounds were designed as estrogen receptor-alpha (ER alpha) coactivator binding Inhibitors. Synthesis was accomplished through a convergent approach, employing Suzuki coupling chemistry to ligate the Individual modular units. Initial biological results support the ability of these compounds to compete for the ER alpha coactivator binding groove.