7-Substituted 2-phenyl-benzofurans as ERβ selective ligands

被引：45

作者：

Collini, MD

Kaufman, DH

Manas, ES

Harris, HA

Henderson, RA

Xu, ZB

Unwalla, RJ

Miller, CP

机构：

[1] Wyeth Ayerst Res, Chem & Screening Sci, Collegeville, PA 19426 USA

[2] Wyeth Ayerst Res, Chem & Screening Sci, Cambridge, MA 02140 USA

[3] Wyeth Ayerst Res, Womens Hlth Res Inst, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 19期

关键词：

D O I：

10.1016/j.bmcl.2004.07.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-(4-hydroxy-phenyl)-benzofuran-5-ols with relatively lipophilic groups in the 7-position of the benzofuran was prepared and the affinity and selectivity for ERbeta was measured. Many of the analogues were found to be potent and selective ERbeta ligands. Additional modifications at the benzofuran 4-position as well as at the 3'-position of the 2-phenyl group were found to further increase selectivity. Such modifications led to compounds with <10nM potency and >100-fold selectivity for ERbeta. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：4925 / 4929

页数：5

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