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N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: Novel potent inhibitors of VEGF receptors I and II

Bioorganic & Medicinal Chemistry Letters(2006)

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摘要
Novel potent derivatives of 4-(azolylethyl)thiazole-5-carboxamides are described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity reaching IC50<100nM in both enzymatic and cell-based phosphorylation assays. The compounds also inhibit the related tyrosine kinase, VEGFR-1, with similar potencies.
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关键词
Vascular endothelial growth factor receptor 2,Receptor tyrosine kinase,Dual kinase inhibitor,Angiogenesis,4-(Azolylethyl)thiazole-5-carboxamides
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