Author/Authors :
Hidenori Takahashi، نويسنده , , Younes Bekkali، نويسنده , , Alison J. Capolino، نويسنده , , Thomas Gilmore، نويسنده , , Susan E. Goldrick، نويسنده , , Paul V. Kaplita، نويسنده , , Lisa Liu، نويسنده , , Richard M. Nelson، نويسنده , , Donna Terenzio، نويسنده , , Ji Wang، نويسنده , , Ljiljana Zuvela-Jelaska، نويسنده , , John Proudfoot، نويسنده , , Gerald Nabozny، نويسنده , , David Thomson، نويسنده ,
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.
