title: Synthesis of biphenyl proteomimetics as estrogen receptor-alpha coactivator binding inhibitors.
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.
authors.affiliation: Department of Chemistry and Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, USA.
authors.forename: Anna B
authors.initials: AB
authors.lastname: Williams
authors.forename: Patrick T
authors.initials: PT
authors.lastname: Weiser
authors.forename: Robert N
authors.initials: RN
authors.lastname: Hanson
authors.forename: Jillian R
authors.initials: JR
authors.lastname: Gunther
authors.forename: John A
authors.initials: JA
authors.lastname: Katzenellenbogen
mesh_terms: D001665:Binding Sites; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D047628:Estrogen Receptor alpha / Q000187:drug effects*; D006801:Humans; D018716:Molecular Mimicry; D015394:Molecular Structure
chemical_list: D001713:Biphenyl Compounds; D047628:Estrogen Receptor alpha