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

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

doi:10.1016/j.bmcl.2010.01.133

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

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2340-3. doi: 10.1016/j.bmcl.2010.01.133. Epub 2010 Feb 4.

Affiliation

¹ Medicines Research Centre, Verona, Italy.

PMID: 20202837
DOI: 10.1016/j.bmcl.2010.01.133

Abstract

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.

MeSH terms

Animals
Rats
Receptors, Glucocorticoid / antagonists & inhibitors*
Receptors, Glucocorticoid / metabolism*
Small Molecule Libraries / chemistry*
Small Molecule Libraries / metabolism
Small Molecule Libraries / pharmacology*
Structure-Activity Relationship

Substances

Receptors, Glucocorticoid
Small Molecule Libraries