The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

• Published in: Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2340-2343
• Main Authors: Rimland, Joseph, Dunne, Angela, Hunjan, Suchete S., Sasse, Rosemary, Uings, Iain, Montanari, Dino, Caivano, Matilde, Shah, Poonam, Standing, David, Gray, David, Brown, David, Cairns, William, Trump, Ryan, Smith, Paul W., Bertheleme, Nicolas, D’Alessandro, Pier, Gul, Sheraz, Vimal, Mythily, Smith, David N., Watson, Stephen P.
• Format: Article
• Language: English
• Subjects: Animals; Biological and medical sciences; Glucocorticoid receptor; Glucocorticoid receptor antagonist; GR antagonist; Hormones. Endocrine system; Medical sciences; Pharmacology. Drug treatments; Rats; Receptors, Glucocorticoid - antagonists & inhibitors; Receptors, Glucocorticoid - metabolism; Small Molecule Libraries - chemistry; Small Molecule Libraries - metabolism; Small Molecule Libraries - pharmacology; Structure-Activity Relationship
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2010.01.133

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