Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377526 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
We have recently reported the discovery of a novel class of glucocorticoid receptor (GR) antagonists, exemplified by 3, containing a 1,2-dihydroquinoline molecular scaffold. Further SAR studies of these antagonists uncovered chemical modifications conveying agonist functional activity to this series. These agonists exhibit good GR binding affinity and are selective against other nuclear hormone receptors.
Graphical abstractThe SAR study of novel class of glucocorticoid receptor agonist is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Hidenori Takahashi, Younes Bekkali, Alison J. Capolino, Thomas Gilmore, Susan E. Goldrick, Paul V. Kaplita, Lisa Liu, Richard M. Nelson, Donna Terenzio, Ji Wang, Ljiljana Zuvela-Jelaska, John Proudfoot, Gerald Nabozny, David Thomson,