期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 12, 页码 3333-3338出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.039
关键词
Staurosporine; Protein kinases; Natural products; Ring closing metathesis; Immune system
The synthesis and biological evaluation of JAK3 based staurosporine compounds is described. The compounds are constructed completely de novo, and a ring closing metathesis strategy is used to assemble the sugar mimetic portion. These analogs show potent JAK3 activity against isolated enzyme and in T-cells. One analog (32) showed unique biological effects during in vitro and in vivo tests including inhibition of STAT5 phosphorylation, blockade of mast cell responses, and reduction of JAK3 based effects in mice models of allergic disease. (C) 2009 Elsevier Ltd. All rights reserved.
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