Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor α/β agonist scaffold

被引：37

作者：

Hamann, LG

Meyer, JH

Ruppar, DA

Marschke, KB

Lopez, FJ

Allegretto, EA

Karanewsky, DS

机构：

[1] Ligand Pharmaceut, Dept Med Chem, San Diego, CA 92121 USA

[2] Ligand Pharmaceut, Dept New Leads Discovery, San Diego, CA 92121 USA

[3] Ligand Pharmaceut, Dept Pharmacol, San Diego, CA 92121 USA

[4] Ligand Pharmaceut, Dept Endocrine Biol, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 05期

关键词：

estrogen receptor; osteoporosis;

D O I：

10.1016/j.bmcl.2004.12.077

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An oxabicyclic template for estrogen receptor alpha and beta agonists has been identified which can be tuned to provide moderate levels of selectivity for either receptor sub-type. Structure-activity relationships within this phenol-substituted oxabicyclo[3.3.1]nonene series are described. Select compounds from the present series showed activity in vivo after oral dosing in rodent models of uterine proliferation. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：1463 / 1466

页数：4

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