Your browser version may not work well with NCBI's Web applications. More information here...
1: Bioorg Med Chem Lett. 2007 Jan 15;17(2):326-31. Epub 2006 Oct 26.Click here to read Links

Simplified staurosporine analogs as potent JAK3 inhibitors.

Yang SM, Malaviya R, Wilson LJ, Argentieri R, Chen X, Yang C, Wang B, Cavender D, Murray WV.

Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. syang9@prdus.jnj.com

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.

PMID: 17088059 [PubMed - indexed for MEDLINE]