4-Anilinoquinazoline derivatives

Abstract

An attractive antitumour strategy is to target tumour vasculature, either killing it or preventing its further growth, as it is presumably a normal tissue, and may well be easier to inhibit than the tumour itself. Experiments with endostatin, an endogenous angiogenesis suppressor, suggest that such an approach may well work. Growth factor receptors, particularly those for vascular endothelial growth factor (VEGF), appear to be essential in neovascularisation of tumours. This application reveals 4-anilinoquinazolines, similar to very potent epidermal growth factor receptor (EGFr) tyrosine kinase inhibitors, as very potent and selective VEGFr inhibitors.

• angiogenesis
• anti-tumour
• cancer therapy
• FLT/FLK
• KDR
• quinazoline
• receptor tyrosine kinase inhibitors
• VEGF