Synthesis of biphenyl proteomimetics as estrogen receptor-alpha coactivator binding inhibitors

Org Lett. 2009 Dec 3;11(23):5370-3. doi: 10.1021/ol901999f.

Abstract

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Binding Sites
  • Biphenyl Compounds / chemical synthesis*
  • Biphenyl Compounds / chemistry
  • Biphenyl Compounds / pharmacology
  • Drug Design
  • Estrogen Receptor alpha / drug effects*
  • Humans
  • Molecular Mimicry*
  • Molecular Structure

Substances

  • Biphenyl Compounds
  • Estrogen Receptor alpha