Novel 4-[5-(Substituted-1,2,4-oxadiazol-3-yl)phenylamine] Derivatives of 6,7-Dimethoxy-quinazolines as Potent Inhibitors of VEGF Receptors I and II

摘要

A series of novel 4-[5-(substituted-1,2,4-oxadiazol-3-yl)phenylamine] derivatives at C-4 position of 6,7-dimethoxy-quinazolines were synthesized through multistep synthesis. The new compounds were tested for inhibition of vascular endothelial growth factor receptor II (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity with an IC_(50) as low as 0.017 μM in an HTRF enzymatic assay. Compound 8j exhibited good antibacterial activity by inhibiting the growth of methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-resistant Staphylococcus aureus (MRSA) and ATCC 35218 Escherichia coli (MIC: 0.25-16.00 μg/mL).