2. Academic Validation
  3. Simplified staurosporine analogs as potent JAK3 inhibitors

Simplified staurosporine analogs as potent JAK3 inhibitors

  • Bioorg Med Chem Lett. 2007 Jan 15;17(2):326-31. doi: 10.1016/j.bmcl.2006.10.062.
Shyh-Ming Yang 1,  Ravi Malaviya,  Lawrence J Wilson,  Rochelle Argentieri,  Xin Chen,  Cangming Yang,  Bingbing Wang,  Druie Cavender,  William V Murray
Affiliations

Affiliation

  • 1 Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. [email protected]
PMID: 17088059 DOI: 10.1016/j.bmcl.2006.10.062
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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