Twenty-six　emodin　derivatives　(17　novel)　which　attach　quaternary　ammonium　salt　were　synthesized　and　evaluated　for　their　anticancer　activities　in　vitro　and　in　vivo.　Compounds　11g　+　12g　and　11h　+　12h　had　more　significant　antiproliferative　ability　against　three　cancer　cell　lines　and　low　cytotoxicity　to　HELF.　11g　+　12g　and　11　h　+　12h　induced　AGS　cell　apoptosis　and　arrested　cell　cycle　at　the　G(0)/G(1)　phase　in　a　dose-dependent　manner.　Furthermore,　the　activities　of　the　caspase-3,　-9　enzymes　were　increased　in　the　treated　cells.　In　vivo　studies　revealed　that　compounds　11g　+　12g　and　11h　+　12h　showed　significant　antitumor　activity　compared　with　controlled　group.　(C)　2012　Elsevier　Masson　SAS.　All　rights　reserved.