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

Autor: Ray NC; Argenta Discovery Ltd, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, UK. nick.ray@argentadiscovery.com, Clark RD, Clark DE, Williams K, Hickin HG, Crackett PH, Dyke HJ, Lockey PM, Wong M, Devos R, White A, Belanoff JK
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Sep 01; Vol. 17 (17), pp. 4901-5. Date of Electronic Publication: 2007 Jun 13.
DOI: 10.1016/j.bmcl.2007.06.036
Abstrakt: 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.
Databáze: MEDLINE