Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist

Brown, A. R. et al. (2011) Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist. Bioorganic and Medicinal Chemistry Letters, 21(1), pp. 137-140. (doi:10.1016/j.bmcl.2010.11.054) (PMID:21129964)

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Abstract

High-throughput screening of 3.87 million compounds delivered a novel series of non-steroidal GR antagonists. Subsequent rounds of optimisation allowed progression from a non-selective ligand with a poor ADMET profile to an orally bioavailable, selective, stable, glucocorticoid receptor antagonist.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Goodwin, Dr Richard and Clark, Dr John and Thomson, Dr Fiona
Authors: Brown, A. R., Bosies, M., Cameron, H., Clark, J., Cowley, A., Craighead, M., Elmore, M. A., Firth, A., Goodwin, R., Goutcher, S., Grant, E., Grassie, M., Grove, S. J.A., Hamilton, N. M., Hampson, H., Hillier, A., Ho, K.-K., Kiczun, M., Kingsbury, C., Kultgen, S. G., Littlewood, P. T.A., Lusher, S. J., MacDonald, S., McIntosh, L., McIntyre, T., Mistry, A., Morphy, J. R., Nimz, O., Ohlmeyer, M., Pick, J., Rankovic, Z., Sherborne, B., Smith, A., Speake, M., Spinks, G., Thomson, F., Watson, L., and Weston, M.
College/School:College of Medical Veterinary and Life Sciences > Institute of Cancer Sciences
Journal Name:Bioorganic and Medicinal Chemistry Letters
Publisher:Elsevier
ISSN:0960-894X
ISSN (Online):1464-3405
Published Online:16 November 2010

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