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联苯类蛋白质模拟物的合成及其作为雌激素受体-α共激活剂结合抑制剂的研究。

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

机构信息

Department of Chemistry and Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, USA.

出版信息

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

DOI:10.1021/ol901999f
PMID:19902964
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3263526/
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.

摘要

设计了一系列新型联苯拟肽化合物作为雌激素受体-α（ER(alpha)）共激活子结合抑制剂。合成采用了收敛方法，通过 Suzuki 偶联化学将各个模块单元连接起来。初步的生物学结果表明这些化合物具有竞争 ER(alpha)共激活子结合槽的能力。

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