Details

Autor(en) / Beteiligte

• Roach, Steven L.
• Higuchi, Robert I.
• Adams, Mark E.
• Liu, Yan
• Karanewsky, Donald S.
• Marschke, Keith B.
• Mais, Dale E.
• Miner, Jeffrey N.
• Zhi, Lin

Titel

Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines

Ist Teil von

• Bioorganic & medicinal chemistry, 2008-06, Vol.18 (12), p.3504-3508

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2008

Quelle

MEDLINE

Beschreibungen/Notizen

• 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, receptor selectivity and E-selectin repression activity. 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 ( K i = 1.5 nM) and 100- to 1000-fold selectivity over MR, PR, and AR while showing activity in an E-selectin repression assay.