The invention discloses a polysubstituted benzene compound with biological activity, and a preparation method and an application thereof. The compound provided by the invention has good biological activity, has the activity of inhibiting proliferation of tumor cells, can be used as a lead compound for research and development of a novel drug, and is used for preparation of antitumor drugs, such asdrugs for treating gastric cancer, drugs for treating ovarian cancer, drugs for treating lung cancer and drugs for treating prostate cancer. The synthetic method provided by the invention has the advantages of extensively-available raw materials, simple operation, simple and short route, mild reaction conditions, low cost and potential industrial value.