Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.

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Furet P, Bold G, Hofmann F, Manley P, Meyer T, Altmann KH

Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):2967-71.

PubMed ID

12941313 [ View in PubMed

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Abstract

The vascular endothelial growth factor (VEGF) tyrosine kinase receptors KDR and Flt-1 are targets of current interest in anticancer drug research. PTK787/ZK222584 is a potent inhibitor of these enzymes in clinical evaluation as an antiangiogenic agent. The development of a hypothesis concerning the bioactive conformation of this compound has led to the discovery of a new class of potent inhibitors of KDR and Flt-1, the anthranilamides. This could be achieved with a limited experimental effort, which only involved the testing of one archive compound and the synthesis and testing of one appropriate analogue.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
N-(4-chlorophenyl)-2-[(pyridin-4-ylmethyl)amino]benzamide	Vascular endothelial growth factor receptor 1	IC 50 (nM)	180	N/A	N/A	Details
Vatalanib	Vascular endothelial growth factor receptor 1	IC 50 (nM)	77	N/A	N/A	Details
Vatalanib	Vascular endothelial growth factor receptor 2	IC 50 (nM)	37	N/A	N/A	Details