666726-71-2Relevant academic research and scientific papers
Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists
Takahashi, Hidenori,Bekkali, Younes,Capolino, Alison J.,Gilmore, Thomas,Goldrick, Susan E.,Kaplita, Paul V.,Liu, Lisa,Nelson, Richard M.,Terenzio, Donna,Wang, Ji,Zuvela-Jelaska, Ljiljana,Proudfoot, John,Nabozny, Gerald,Thomson, David
, p. 5091 - 5095 (2008/02/12)
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.
GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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Page 72, (2010/02/06)
Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, Y, and n are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
