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
  • 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.