期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 5, 页码 1440-1444出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.11.033
关键词
vascular endothelial growth factor receptor 2; receptor tyrosine kinase; dual kinase inhibitor; angiogenesis; 4-(azolylethyl)thiazole-5-carboxamides
A novel potent derivatives of hetaryl imidazoles were described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Several compounds display VEGFR-2 inhibitory activity reaching IC50 < 100 nM in both enzymatic and cellular assays, The compounds also inhibit the related tyrosine kinase, VEGFR-1. By controlling the substitution pattern on the 5-carboxamido functionality, both dual and specific VEGFR-2 thiazoles were identified. (C) 2005 Elsevier Ltd. All rights reserved.
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