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The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2010-02-04 , DOI: 10.1016/j.bmcl.2010.01.133
Joseph Rimland , Angela Dunne , Suchete S. Hunjan , Rosemary Sasse , Iain Uings , Dino Montanari , Matilde Caivano , Poonam Shah , David Standing , David Gray , David Brown , William Cairns , Ryan Trump , Paul W. Smith , Nicolas Bertheleme , Pier D’Alessandro , Sheraz Gul , Mythily Vimal , David N. Smith , Stephen P. Watson

The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure–activity relationships and the process of optimisation of an initial HTS hit are also described.



中文翻译:

鉴定新型,选择性,非甾体功能性糖皮质激素受体拮抗剂

描述了对PR有选择性的新型有效非甾体/小分子功能GR拮抗剂GSK1564023A的鉴定。还描述了相关的结构-活性关系和初始HTS命中的优化过程。

更新日期:2010-02-04
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