New　potent　mTORC1/mTORC2　dual　inhibitors,　5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one　derivatives,　were　obtained　by　optimizing　functional　groups　on　our　previously　reported　PI3K　alpha　inhibitor.　All　the　target　compounds　were　synthesized　and　structural　optimization　on　the　structure　of　the　lead　compound　based　on　cytotoxic　activity.　The　results　showed　that　some　of　the　target　compounds　exhibited　moderate　to　high　cytotoxic　activity　against　cell　line　U87MG　and　PC-3.　The　activities　against　mTOR　kinase　were　investigated　and　the　compound　12q　showed　excellent　activity　with　an　IC50　value　of　54　nM　in　the　same　level　of　the　positive　control　BEZ235　with　IC50,　value　of　55　nM　under　the　same　test　conditions.　The　western　blot　and　cell　cycle　results　demonstrate　that　compound　12q　is　a　candidate　as　an　mTORC1/mTORC2　dual-target　inhibitor.　The　theoretical　calculations　were　also　performed　to　better　understanding　the　binding　modes　of　the　compound　12q　in　the　mTOR　active　site.