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

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Kiselyov AS, Piatnitski E, Semenova M, Semenov VV

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

Bioorg Med Chem Lett. 2006 Feb;16(3):602-6. Epub 2005 Nov 3.

PubMed ID

16275072 [ View in PubMed

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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 IC(50)<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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Vatalanib	Vascular endothelial growth factor receptor 1	IC 50 (nM)	140	7.5	22	Details
Vatalanib	Vascular endothelial growth factor receptor 2	IC 50 (nM)	54	7.5	22	Details