2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor

被引：27

作者：

Henke, BR

Drewry, DH

Jones, SA

Stewart, EL

Weaver, SL

Wiethe, RW

机构：

[1] Glaxo Wellcome Res & Dev, Dept Med Chem, Res Triangle Pk, NC 27709 USA

[2] Glaxo Wellcome Res & Dev, Dept Struct Chem, Res Triangle Pk, NC 27709 USA

[3] Glaxo Wellcome Res & Dev, Dept Mol Endocrinol, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(01)00321-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have prepared a novel series of 2-amino-4,6-diarylpyridines that function as ligands of estrogen receptor alpha (ER alpha) and estrogen receptor beta (ER beta). These compounds bind to both ER alpha and ER beta with a modest selectivity for the alpha subtype. The most potent of these analogues, compound 19, has a K-i = 20nM at ER alpha. These molecules represent a novel template for designing potentially useful ligands for the estrogen receptor. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：1939 / 1942

页数：4

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