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Bioorg Med Chem Lett. 2007 Jan 15;17(2):326-31. Epub 2006 Oct 26.

Simplified staurosporine analogs as potent JAK3 inhibitors.

Author information

1
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. syang9@prdus.jnj.com

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.

PMID:
17088059
DOI:
10.1016/j.bmcl.2006.10.062
[Indexed for MEDLINE]

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