Tetrahydro-beta-carbolines　(TH　beta　Cs)　are　a　kind　of　natural　alkaloids　with　multiple　pharmaceutical　activities.　Herein,　a　focused　compound　library　derived　from　TH　beta　Cs　was　synthesized　and　their　anticancer　activities　were　studied　in　several　cancer　cell　lines.　Among　them,　three　compounds　showed　considerable　anticancer　activities　with　low　micromolar　to　submicromolar　IC50　values.　The　abilities　to　induce　apoptosis　and　alter　mitochondrial　membrane　potential　levels,　which　are　comparable　to　those　of　the　commercial　anticancer　drug　adriamycin,　were　confirmed　by　one　representative　compound　(21)　on　the　B16/F10　cell　line.　Our　preliminary　structure-activity　relationship　studies　indicated　that　alkylamines　with　suitable　lengths　are　very　important　for　potency　improvement.