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ID: ALA1136193

Journal: Bioorg Med Chem Lett

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

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

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.

CiteXplore: 12941313

DOI: 10.1016/s0960-894x(03)00626-7