618359-42-5Relevant academic research and scientific papers
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching
Furet, Pascal,Bold, Guido,Hofmann, Francesco,Manley, Paul,Meyer, Thomas,Altmann, Karl-Heinz
, p. 2967 - 2971 (2003)
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.
