Article ID Journal Published Year Pages File Type
1366952 Bioorganic & Medicinal Chemistry Letters 2007 6 Pages PDF
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.

Graphical abstractThe modification of staurosporine led to a new series of potent JAK3 inhibitors is described.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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