(1,2,3-Triazol-4-yl)benzenamines: synthesis and activity against VEGF receptors 1 and 2

Alexander S Kiselyov; Marina Semenova; Victor V Semenov

doi:10.1016/j.bmcl.2009.01.046

(1,2,3-Triazol-4-yl)benzenamines: synthesis and activity against VEGF receptors 1 and 2

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1344-8. doi: 10.1016/j.bmcl.2009.01.046. Epub 2009 Jan 20.

Authors

Alexander S Kiselyov¹, Marina Semenova, Victor V Semenov

Affiliation

¹ deCODE, 2501 Davey Road, Woodridge, IL 60517, USA.

PMID: 19188066
DOI: 10.1016/j.bmcl.2009.01.046

Abstract

Derivatives of (1,2,3-triazol-4-yl)benzenamines are described as potent and ATP-competitive inhibitors of vascular endothelial growth factor receptors I and II (VEGFR-1/2). A number of compounds exhibited VEGFR-2 and VEGFR-1 inhibitory activity comparable to that of Vatalanib in both HTRF enzymatic and cellular assays.

Publication types

Comparative Study

MeSH terms

Benzene Derivatives / chemical synthesis*
Benzene Derivatives / pharmacology*
Binding Sites / drug effects
Humans
Triazoles / chemical synthesis*
Triazoles / pharmacology*
Vascular Endothelial Growth Factor Receptor-1 / antagonists & inhibitors*
Vascular Endothelial Growth Factor Receptor-1 / metabolism
Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*
Vascular Endothelial Growth Factor Receptor-2 / metabolism

Substances

1,3-di(1,2,3-triazol-4-yl)benzene
Benzene Derivatives
Triazoles
Vascular Endothelial Growth Factor Receptor-1
Vascular Endothelial Growth Factor Receptor-2