Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands

被引：27

作者：

Fang, Jing ^{[1
]}

Akwabi-Ameyaw, Adwoa ^{[1
]}

Britton, Jonathan E. ^{[1
]}

Katamreddy, Subba R. ^{[1
]}

Navas, Frank, III ^{[1
]}

Miller, Aaron B. ^{[1
]}

Williams, Shawn P. ^{[1
]}

Gray, David W. ^{[1
]}

Orband-Miller, Lisa A. ^{[1
]}

Shearin, Jean ^{[1
]}

Heyer, Dennis ^{[1
]}

机构：

[1] GlaxoSmithKline Res, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 18期

关键词：

estrogen receptor ligands; ER binding; naphthalene;

D O I：

10.1016/j.bmcl.2008.07.121

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of estrogen receptor ligands based on a 3-alkyl naphthalene scaffold was synthesized using an intramolecular enolate-alkyne cycloaromatization as the key step. Several of these compounds bearing a C6-OH group were shown to be high affinity ligands. All compounds had similar ER alpha and ER beta binding affinity ranging from micromolar to low nanomolar. (C) 2008 Elsevier Ltd. All rights reserved.

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收藏

页码：5075 / 5077

页数：3

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