The invention relates to the application of marine biological metabolite Tagalsin C and its homologues Tagalsins A, B, D, E, F, G in the preparation of antitumor drugs. This series of compounds has membrane permeability and broad-spectrum anti-tumor activity, and can kill human promyelocytic acute leukemia cells HL-60, human myeloma cells IM9, human acute T-cell leukemia cells Jurkat, and human macrophage lymphoma cells U937, human lung cancer cell A549, human breast cancer cell MCF-7 and MDA-MB-231, human liver cancer cell HepG2, human prostate cancer cell PC-3 and human cervical cancer epithelial cell Hela, while normal cell human kidney blast 293 And the human liver diploid cell L02 has no obvious killing ability, and can be applied to the preparation of drugs for treating tumors, drugs for treating clinical high expression of Bcl-2, resistant to conventional chemotherapy, and drugs for treating recurrent cancer.