Title of article :
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines
Author/Authors :
Steven L. Roach، نويسنده , , Robert I. Higuchi، نويسنده , , Mark E. Adams، نويسنده , , Yan Liu، نويسنده , , Donald S. Karanewsky، نويسنده , , Keith B. Marschke، نويسنده , , Dale E. Mais، نويسنده , , Jeffrey N. Miner، نويسنده , , Lin Zhi، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Abstract :
A series of nonsteroidal glucocorticoid receptor (GR) ligands based on a 6-indole-1,2,3,4-tetrahydroquinoline scaffold are reported. Structure–activity relationship (SAR) of the pendent indole group identified compound 20 exhibiting good GR binding affinity (Ki = 1.5 nM) and 100- to 1000-fold selectivity over MR, PR, and AR while showing activity in an E-selectin repression assay.
Keywords :
inflammation , prednisolone , Glucocorticoid receptor , E-selectin
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
