Abstract
Alpha-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 30 nM binding to hGR. The SAR and selectivity of these compounds will be discussed.
MeSH terms
-
Drug Design
-
Drug Evaluation, Preclinical
-
Humans
-
Ligands
-
Receptors, Glucocorticoid / drug effects*
-
Receptors, Mineralocorticoid / drug effects
-
Receptors, Progesterone / drug effects
-
Stereoisomerism
-
Structure-Activity Relationship
-
Sulfonamides / chemical synthesis*
-
Sulfonamides / pharmacology*
-
Tryptamines / chemical synthesis*
-
Tryptamines / pharmacology*
Substances
-
Ligands
-
Receptors, Glucocorticoid
-
Receptors, Mineralocorticoid
-
Receptors, Progesterone
-
Sulfonamides
-
Tryptamines
-
alpha-methyltryptamine sulfonamide