Hetaryl imidazoles: A novel dual inhibitors of VEGF receptors I and II

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• 作者：Alexander S. Kiselyov ; Marina Semenova and Victor V. Semenov
• 关键词：Vascular endothelial growth factor receptor 2 ; Receptor tyrosine kinase ; Dual kinase inhibitor ; Angiogenesis ; 4-(Azolylethyl)thiazole-5-carboxamides
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 March 2006
• 年：2006
• 卷：16
• 期：5
• 页码：1440-1444
• 全文大小：118 K

文摘

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.