The invention provides a substituted benzofuran derivative. A chemical structure of the derivative is as shown in general formula I. The invention further provides a preparation method of the formulaI, the preparation method is as shown in the following reaction formula described in the specification, wherein R and R' are defined the same as the specification. In-vitro proliferation inhibition experiment researches of human tumor cells show that the substituted benzofuran derivative has excellent inhibition effects on tumor cells such as human hepatoma cells HLF, human intestinal cancer cellsHCT116, human breast cancer cells MDA-MB-231, human prostate cancer cells DU145, human melanoma cells A375, human colon cancer cells Lovo, human kidney cancer cells 786-o, human chronic myeloid leukemia cells K562, human gastric cancer cells MGC-803, human pancreatic cancer cells PANC-1, can be used for preparing an anti-tumor drug, has low acute toxicity and good water solubility, and has good clinical application prospects. The preparation method provided by the invention is suitable for industrial production.