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α-Methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands

Authors :
Marshall, Daniel R.
Rodriguez, Gus
Thomson, David S.
Nelson, Richard
Capolina, Allison
Source :
Bioorganic & Medicinal Chemistry Letters. Jan2007, Vol. 17 Issue 2, p315-319. 5p.
Publication Year :
2007

Abstract

Abstract: α-Methyltryptamine sulfonamides were identified as human glucocorticoid receptor (hGR) ligands in an ultra high throughput screening (UHTS) campaign. Described will be the hit-to-lead activities, including parallel and single point analog synthesis to map the scaffold. Ligands were identified that exhibited 30nM binding to hGR. The SAR and selectivity of these compounds will be discussed. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
17
Issue :
2
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
23671034
Full Text :
https://doi.org/10.1016/j.bmcl.2006.10.058