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
收藏
页码：1527 / 1531
页数：5
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