The　anticancer　efficacy　of　ursolic　acid　(UA)　was　limited　by　poor　water　solubility,　non-specific　tumor　distribution,　and　low　bioavailability.　To　overcome　this　problem,　polyamidoamine　(PAMAM)　conjugated　with　UA　and　folic　acid　(FA)　as　novel　dendrimeric　prodrugs　were　designed　and　successfully　synthesized　by　a　concise　one-pot　synthetic　approach.　Both　FA　and　UA　were　covalently　conjugated　to　the　surface　of　PAMAM　through　acid-labile　ester　bonds　and　the　covalently　linked　UA　could　be　hydrolysed　either　in　acidic　(pH　5.4)　or　in　neutral　(pH　7.4)　PBS　solution.　The　cellular　uptake　study　indicated　that　the　presence　of　FA　enhanced　uptake　of　the　dendrimeric　prodrugs　in　folate　receptor　(FR)　over-expressing　Hela　cells.　The　enhanced　cellular　uptake　could　be　due　to　the　electrostatic　absorptive　endocytosis　and　FR-mediated　endocytosis.　In　contrast,　for　HepG2　cells,　a　FR-negative　cell　line,　FA　conjugation　on　the　surface　of　the　dendrimer　showed　no　effect　on　the　cellular　uptake.　In　MTT　assay　and　cell　cycle　analysis,　FA-modified　dendrimeric　prodrugs　showed　significantly　enhanced　toxicity　than　non-FA-modified　ones　in　Hela　cells.　These　results　suggested　that　FA-modified　dendrimeric　UA　prodrugs　have　the　potential　for　targeted　delivery　of　UA　into　cancer　cells　to　improve　its　anti-tumor　efficacy.　©　2015　Elsevier　B.V.　All　rights　reserved.