Abstract: The metabolites produced by complex and diverse microorganisms are important resources for drug research and development. Using new targets to screen microbial metabolites, many anti-cancer drugs acting on different targets are discovered. Anti-tumor antibiotics acting on various targets and signaling pathways are important members in the study of specific targets for anti-tumor, and some anticancer antibiotics with potent antitumor activity are used as "warheads" of antibody-drug conjugates. Microbial-derived anti-tumor substances acting on different targets with high-efficiency "warheads" molecules are reviewed to provide a literature basis for research on the anti-cancer drugs for specific targets derived from microorganisms.