Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.
Article Details
- CitationCopy to clipboard
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]
- 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