Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 11, Issue 18, Pages 3869-3878Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0968-0896(03)00438-3
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In this study, we have investigated the roles of substituents on the terminal phenyl ring at the C(4)-position of the quinazoline core to complete the structure-activity relationships (SARs) of our NF-kappaB activation inhibitors. Among them, compound 12j afforded highly potent inhibitory activity toward NF-kappaB transcriptional activation with IC50 value of 2nM, along with an excellent in vivo efficacy by reducing the edema formation seen in carrageenin-induced inflammation of the rat hind paw. (C) 2003 Elsevier Ltd. All rights reserved.
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