| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373342 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
Starting from a non-steroidal glucocorticoid agonist aryl pyrazole derivative, the NFκB agonist activity was optimised in an iterative process from pIC50 7.5 (for 7), to pIC50 10.1 (for 38E1). An explanation for the SAR observed based is presented along with a proposed docking of 38E1 into the active site of the glucocorticoid receptor.
Graphical abstractThe discovery of 38E1 as a highly potent non-steroidal glucocorticoid agonist is described.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Keith Biggadike, Matilde Caivano, Margaret Clackers, Diane M. Coe, George W. Hardy, Davina Humphreys, Haydn T. Jones, David House, Annette Miles-Williams, Philip A. Skone, Iain Uings, Vicki Weller, Iain M. McLay, Simon J.F. Macdonald,