Simplified staurosporine analogs as potent JAK3 inhibitors |
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| Authors: | Yang Shyh-Ming Malaviya Ravi Wilson Lawrence J Argentieri Rochelle Chen Xin Yang Cangming Wang Bingbing Cavender Druie Murray William V |
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| Affiliation: | Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. syang9@prdus.jnj.com |
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| 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. |
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