Simplified staurosporine analogs as potent JAK3 inhibitors

Simplification of bottom ring and regioselective functionalization of the indolocarbazole unit of staurosporine (2) are described. The modification led to a new series of simplified staurosporine analogs, which exhibited significant inhibitory activity against Janus kinase 3 (JAK3). The structure–activity relationships (SAR) are discussed and a proposed binding model is also highlighted.

The modification of staurosporine led to a new series of potent JAK3 inhibitors is described.Figure optionsDownload as PowerPoint slide