To　obtain　new　anticancer　agents　with　antimetastatic　adjunct　efficacy,　a　series　of　novel　N-4-hydrazone　derivatives　of　5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one　were　designed　and　synthesized　by　an　eight-step　reaction,　with　appropriate　yields.　All　the　synthesized　compounds　were　evaluated　for　their　antiproliferative　activity　against　A549　and　MCF-7　cells　and　for　antiplatelet　aggregation　activity　in　vitro.　The　results　showed　that　compounds　25　and　35　not　only　showed　potent　antiproliferative　activity　against　the　A549　(IC50　=　15.3　and　21.4　mu　M)　and　MCF-7　(IC50　=　15.6　and　10.9　mu　M)　cell　lines　but　also　showed　certain　antiplatelet　aggregation　activity　(inhibition　rates:　47.0%　and　45.8%).　These　results　indicated　that　the　structural　modification　on　the　N-4-hydrazone　moiety　of　5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one　is　promising　to　obtain　novel　anticancer　compounds　with　antimetastatic　adjunct　efficacy.　In　addition,　a　molecular　docking　study　was　performed　to　investigate　the　possible　targets,　and　these　results　indicated　that　compounds　25　and　35　have　the　potential　to　target　EGFR,　HER2,　and　P2Y(12).