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Even though there are a number of therapeutic agents against cancer, compounds from natural sources remain the first choice as therapeutic agents. Numerous studies have now shown natural products and their roles in treating cancer. Fungi are microbes that have not been extensively explored, and they have numerous secondary metabolites that have anticancer potential. Fungi are excellent producers of natural products of therapeutic potential. Fungi are the natural producers of structurally diverse metabolites of highly diverse classes such as amino acids, anthracenones, aromatic compounds, butenolides, butanolides, cytochalasans, pyrones, naphthalenones, terpenes, and macrolides. It has become evident to explore secondary metabolites of fungal origin with promising anticancer activities. In this chapter, our focus is to highlight the potential of fungi as a natural producer of secondary metabolites with …