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

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• 作者：Anna B. Williams ; Patrick T. Weiser ; Robert N. Hanson ; Jillian R. Gunther ; John A. Katzenellenbogen
• 刊名：Organic Letters
• 出版年：2009
• 出版时间：December 3, 2009
• 年：2009
• 卷：11
• 期：23
• 页码：5370-5373
• 全文大小：164K
• 年卷期：v.11,no.23(December 3, 2009)
• ISSN：1523-7052

文摘

A novel series of biphenyl proteomimetic compounds were designed as estrogen receptor-α (ER_α) 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_α coactivator binding groove.