Synthesis of biphenyl proteomimetics as estrogen receptor-alpha 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.
Williams
Anna B
AB
Department of Chemistry and Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, USA.
Weiser
Patrick T
PT
Hanson
Robert N
RN
Gunther
Jillian R
JR
Katzenellenbogen
John A
JA
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
D001713:Biphenyl Compounds; D047628:Estrogen Receptor alpha