Fourteen　benzofuran-isatin　hybrids　6a-f　and　7a-h　tethered　via　alkyl　linker　(pentylene　and　hexylene)　were　designed　and　synthesized,　and　hybrids　6c-f　and　7a-h　were　screened　for　their　in　vitro　anticancer　activity　against　various　human　cancer　cell　lines.　The　majority　of　the　hybrids　were　active　against　the　tested　cancer　cells,　and　the　most　active　hybrids　7g　(half　maximal　inhibitory　concentration/IC50:　77.2-88.9　mu　M)　and　7h　(IC50:　65.4-89.7　mu　M),　which　possessed　broad　spectrum　anticancer　activity　were　as　potent　as　the　reference　vorinostat　(IC50:　64.2-＞100　mu　M)　against　all　tested　cancer　cell　lines,　could　act　as　leads　for　further　investigations.　The　structure-activity　relationship　is　also　discussed,　and　the　enriched　structure-activity　relationship　may　afford　useful　information　for　further　rational　design　of　the　candidates　with　higher　activity.