Discovery of quinolines as selective glucocorticoid receptor agonists

被引：18
|
作者：
Jaroch, Stefan [1 ]
Berger, Markus [1 ]
Huwe, Christoph [1 ]
Krolikiewicz, Konrad [1 ]
Rehwinkel, Hartmut [1 ]
Schaecke, Heike [2 ]
Schmees, Norbert [1 ]
Skuballa, Werner [1 ]
机构：
[1] Bayer Schering Pharma AG, Med Chem Berlin, Lead Generat & Optimizat, D-13342 Berlin, Germany
[2] Bayer Schering Pharma AG, Global Therapeut Res, Common Mech Res Berlin, D-13342 Berlin, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 19期
关键词：
Glucocorticoid; SEGRA; Transrepression; Transactivation; Quinoline; IN-VITRO PROFILE; A-RING MIMETICS; MODULATORS; LIGANDS; MECHANISMS; BINDING; TRANSACTIVATION; TRANSREPRESSION; IDENTIFICATION; SUBSTITUTION;
D O I：
10.1016/j.bmcl.2010.07.125
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The dissociated glucocorticoid receptor (GR) agonist ZK 216348 is rendered GR-selective over other nuclear hormone receptors through replacing the methylbenzoxazine with a quinoline moiety. Compounds were shown to be efficacious in cell assays with respect to inflammation endpoints, along with reduced activity in a transactivation assay, hinting at an improved therapeutic window over corticosteroids. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5835 / 5838
页数：4
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