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
Pages
5
From page
3504
To page
3508
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
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799586
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