Epidermal　growth　factor　receptor　(EGFR)　kinase　is　a　promising　target　for　the　development　of　novel　anticancer　drugs.　Based　on　the　structure-activity　relationships　for　the　known　inhibitors,　3,9-diazatetraasteranes　have　been　developed　as　novel　EGFR　inhibitors.　Molecular　docking　is　performed　for　3,9-diazatetraasteranes　and　the　known　inhibitor　Erlotinib,　and　it　suggests　that　3,9-diazatetraasteranes　are　similar　to　Erlotinib　in　interactions　with　the　catalytic　sites　of　EGFR.　A　series　of　3,9-diazatetraasteranes　has　been　synthesized　by　photocyclization　of　4-atyl-1,4-dihydropyridines,　and　their　biological　activity　has　been　evaluated　against　A431　and　HepG2　cell　lines　using　Erlotinib　as　a　control.　Compound　1c　exhibits　the　most　potent　antiproliferative　activity　against　A431　(IC50　=　7.37　mu　M)　and　HepG2　(IC50　=　9.81　mu　M)　cell　lines　compared　to　positive　controls　(IC50　=　8.92　mu　M　and　12.08　mu　M).　The　results　are　indicating　that　3,9-diazatetraasteranes　may　be　the　promising　potential　EGFR　inhibitors.