Title of article :
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists
Author/Authors :
Irini Akritopoulou-Zanze، نويسنده , , Jyoti R Patel، نويسنده , , Kresna Hartandi، نويسنده , , Jehrod Brenneman، نويسنده , , Martin Winn، نويسنده , , John K Pratt، نويسنده , , Marlene Grynfarb، نويسنده , , Annika Goos-Nisson، نويسنده , , Thomas W von Geldern، نويسنده , , Philip R Kym، نويسنده ,
Abstract :
We report the discovery of a novel class of glucocorticoid receptor (GR) antagonists based on the chromene molecular scaffold. The compounds exhibit good functional potency and an improved receptor selectivity profile for GR over other steroid receptors when compared to the classical steroidal GR-antagonist, RU-486.