Novel selective androgen receptor modulators:: SAR studies on 6-bisalkylamino-2-quinolinones

被引：21

作者：

van Oeveren, Arjan ^{[1
]}

Motamedi, Mehrnoush ^{[1
]}

Martinborough, Esther ^{[1
]}

Zhao, Shuo ^{[1
]}

Shen, Yixing ^{[1
]}

West, Sarah ^{[1
]}

Chang, William ^{[1
]}

Kallel, Adam ^{[1
]}

Marschke, Keith B. ^{[1
]}

Lopez, Francisco J. ^{[1
]}

Negro-Vilar, Andres ^{[1
]}

Zhi, Lin ^{[1
]}

机构：

[1] Ligand Pharmaceut Inc, Discovery Res, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 06期

关键词：

androgen receptor; SARM; 2-quinolinone; AR agonist;

D O I：

10.1016/j.bmcl.2007.01.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of selective androgen receptor modulators (SARMs) with a wide spectrum of receptor modulating activities was developed based on optimization of the 4-substituted 6-bisalkylamino-2-quinolinones (3). Significance of the trifluoromethyl group on the side chains and its interactions with amino acid residues within the androgen receptor (AR) ligand binding domain are discussed. A representative analog (9) was tested orally in a rodent model of hypogonadism and demonstrated desirable tissue selectivity. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：1527 / 1531

页数：5

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