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.
MeSH terms
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Adenosine Triphosphate / metabolism
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Indicators and Reagents
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Janus Kinase 3 / antagonists & inhibitors*
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Models, Molecular
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Protein Binding
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Staurosporine / analogs & derivatives*
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Staurosporine / pharmacology*
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Indicators and Reagents
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Adenosine Triphosphate
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Janus Kinase 3
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Staurosporine