Disclosed are a multi-substituted benzene compound having biological activity, a preparation method therefor, and an application thereof. The compound of the present invention has good biological activity and the activity of inhibiting tumor cell proliferation, and can be used as a lead compound for the research and development of novel drugs and for the preparation of anti-tumor drugs, such as drugs for the treatment of gastric cancer, ovarian cancer, lung cancer, or prostate cancer. The synthesis method of the present invention has wide availability of raw materials, ease of operation, short route, mild reaction conditions, low costs, and a potential value for industrialization.