Author/Authors :
Shyh-Ming Yang، نويسنده , , Ravi Malaviya، نويسنده , , Lawrence J. Wilson، نويسنده , , Rochelle Argentieri، نويسنده , , Xin Chen، نويسنده , , Cangming Yang، نويسنده , , Bingbing Wang، نويسنده , , Druie Cavender، نويسنده , , William V. Murray، نويسنده ,
Abstract :
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.