Starting　with　our　previously　reported　work,　a　novel　series　of　3,4-dihydro-2H-[1,4]oxazino[2,3-f]quinazolin-derivatives　were　designed,　synthesized　and　evaluated　as　potent　EGFR　tyrosine　kinase　inhibitors.　All　of　the　compounds　showed　significant　inhibitory　activities　against　EGFRwt　kinase　(IC50　＜=　937.7　nM).　Among　them,　compound　7j　demonstrated　the　most　potent　inhibitory　activity　toward　EGFRwt　tyrosine　kinase　with　IC50　value　of　25.69　nM　and　showed　good　antiproliferative　activities　against　NCI-H1563　and　H1975　cells.　The　median　cytotoxic　concentration　(CC50)　showed　that　most　of　the　tested　compounds　displayed　almost　no　cytotoxicity　in　vitro　against　16HBE　cells.　In　view　of　the　reported　compounds　activity,　the　structure　deserves　further　optimization　as　cancer　treatment　agents.