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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.

SUBMITTER: Williams AB 

PROVIDER: S-EPMC3263526 | biostudies-literature | 2009 Dec

REPOSITORIES: biostudies-literature

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

Williams Anna B AB   Weiser Patrick T PT   Hanson Robert N RN   Gunther Jillian R JR   Katzenellenbogen John A JA  

Organic letters 20091201 23

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. ...[more]

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