α-Methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands

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 30 nM binding to hGR. The SAR and selectivity of these compounds will be discussed.

Graphical abstractα-Methyltryptamine sulfonamides were identified as human glucocorticoid receptor (hGR) ligands. The SAR and selectivity will be discussed.Figure optionsDownload full-size imageDownload as PowerPoint slide