期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 23, 页码 6067-6072出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.08.102
关键词
Tp12 kinase; quinoline-3-carbonitrile
The synthesis and structure-activity studies of a series of quinoline-3-carbonitriles as inhibitors of Tp12 kinase are described. Potent inhibitors of Tp12 kinase with selectivity against a panel of selected kinases in enzymatic assays and specificity in cell-based phosphorylation assays in LPS-treated human monocytes were identified. Selected inhibitors with moderate activity in human whole blood assay effectively inhibited LPS/D-Gal induced TNF alpha release when administered intraperitoneally in mice. (c) 2006 Elsevier Ltd. All rights reserved.
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