Background: Fungi are a well-known and valuable source of compounds of therapeutic relevance,
in particular of novel anticancer compounds. Although seldom obtainable through isolation from
the natural source, the total organic synthesis still remains one of the most efficient alternatives to resupply
them. Furthermore, natural product total synthesis is a valuable tool not only for discovery of
new complex biologically active compounds but also for the development of innovative methodologies
in enantioselective organic synthesis.
Methods: We undertook an in-depth literature searching by using chemical bibliographic databases
(SciFinder, Reaxys) in order to have a comprehensive insight into the wide research field. The literature
has been then screened, refining the obtained results by subject terms focused on both biological activity
and innovative synthetic procedures.
Results: The literature on fungal metabolites has been recently reviewed and these publications have
been used as a base from which we consider the synthetic feasibility of the most promising compounds,
in terms of anticancer properties and drug development. In this paper, compounds are classified according
to their chemical structure.
Conclusion: This review summarizes the anticancer potential of fungal metabolites, highlighting the
role of total synthesis outlining the feasibility of innovative synthetic procedures that facilitate the development
of fungal metabolites into drugs that may become a real future perspective. To our knowledge,
this review is the first effort to deal with the total synthesis of these active fungi metabolites and
demonstrates that total chemical synthesis is a fruitful means of yielding fungal derivatives as aided by
recent technological and innovative advancements.