
pmid: 17088059
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.
Models, Molecular, Structure-Activity Relationship, Adenosine Triphosphate, Janus Kinase 3, Indicators and Reagents, Enzyme Inhibitors, Staurosporine, Protein Binding
Models, Molecular, Structure-Activity Relationship, Adenosine Triphosphate, Janus Kinase 3, Indicators and Reagents, Enzyme Inhibitors, Staurosporine, Protein Binding
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