Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators

…, DE Clark, K Williams, HG Hickin, PH Crackett…

Index: Ray, Nicholas C.; Clark, Robin D.; Clark, David E.; Williams, Karen; Hickin; Crackett, Peter H.; Dyke, Hazel J.; Lockey, Peter M.; Wong, Melanie; Devos, Rene; White, Anne; Belanoff, Joseph K. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 17 p. 4901 - 4905

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Citation Number: 26

Abstract

A virtual screening approach comprising a 3-D similarity search based on known GR modulators was used to identify a novel series of non-steroidal glucocorticoid receptor (GR) antagonists. Optimization of the initial hit to provide potent compounds which exhibit good selectivity against other steroidal nuclear hormone receptors is described.