3,4-Dihydroquinazolin-8-yl-3-phenylurea Derivatives: Synthesis, VEGFR-2 Kinase Inhibiting Activity, and Molecular Docking

New 15 compounds have been synthesized targeting the highly conserved active site of VEGFR-2. Some of those have exhibited high anti-proliferation potency against tumor cells and inhibitory activity against VEGFR-2. One of the products (6h) has displayed the most efficient cytotoxic activity against Hela cell line in vitro (IC50 = 6.10 μM) and VEGFR-2 kinase activity (IC50 = 483.1 nM). Molecular docking analysis has indicated 6h as a Type-II inhibitor of VEGFR-2 kinase. In general, the accumulated data prove 3,4-dihydroquinazolin-8-yl-3-phenylurea derivatives to be promising inhibitors of VEGFR-2 for the potential treatment of anti-angiogenesis.