Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.
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.
Marshall
Daniel R
DR
Boehringer Ingelheim Pharmaceuticals, Inc. 900 Ridgebury Rd/PO Box 368, Ridgefield, CT 06877-0368, USA. dmarshal@rdg.boehringer-ingelheim.com
Rodriguez
Gus
G
Thomson
David S
DS
Nelson
Richard
R
Capolina
Allison
A
D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008024:Ligands; D011965:Receptors, Glucocorticoid / Q000187:drug effects*; D018161:Receptors, Mineralocorticoid / Q000187:drug effects; D011980:Receptors, Progesterone / Q000187:drug effects; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D014363:Tryptamines / Q000138:chemical synthesis* / Q000494:pharmacology*
D008024:Ligands; D011965:Receptors, Glucocorticoid; D018161:Receptors, Mineralocorticoid; D011980:Receptors, Progesterone; D013449:Sulfonamides; D014363:Tryptamines; C518581:alpha-methyltryptamine sulfonamide