Title of article
N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: Novel potent inhibitors of VEGF receptors I and II
Author/Authors
Alexander S. Kiselyov، نويسنده , , Evgueni Piatnitski، نويسنده , , Marina Semenova، نويسنده , , Victor V. Semenov، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
602
To page
606
Abstract
Novel potent derivatives of N-(aryl)-4-(azolylethyl)thiazole-5-carboxamides are 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 pharmacophore, both dual and specific VEGFR-2 thiazoles were identified.
Keywords
Vascular endothelial growth factor receptor 2 , Dual kinase inhibitor , Receptor tyrosine kinase , angiogenesis , 4-(Azolylethyl)thiazole-5-carboxamides
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796424
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