期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 24, 页码 7367-7372出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.10.025
关键词
Protein Kinase C; Inhibitors; Isozyme specific; 2,6-Naphthyridines; T cell inhibition
The present study describes a novel series of ATP-competitive PKC inhibitors based on the 2,6-naphthyridine template. Example compounds potently inhibit the novel Protein Kinase C (PKC) isotypes delta, epsilon, eta, theta (in particular PKC epsilon/eta, and display a 10-100-fold selectivity over the classical PKC isotypes. The prototype compound 11 was found to inhibit PKC theta-dependent pathways in vitro and in vivo. In vitro, a-CD3/a-CD28-induced lymphocyte proliferation could be effectively blocked in 10% rat whole blood. In mice, 11 dose-dependently inhibited Staphylococcus aureus enterotoxin B-triggered IL-2 serum levels after oral dosing. (C) 2011 Elsevier Ltd. All rights reserved.
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