Microorganisms still remain the main hotspots in the global drug discovery avenue. In particular, fungi are highly prolific producers of vast structurally diverse specialized secondary metabolites, which have displayed a myriad of biomedical potentials. Intriguingly, isocoumarins is one distinctive class of fungal natural products polyketides, which demonstrated numerous remarkable biological and pharmacological activities. This review article provides a comprehensive state-of-the-art over the period 2000-2022 about the discovery, isolation, classifications, and therapeutic potentials of isocoumarins exclusively reported from fungi. Indeed, a comprehensive list of 351 structurally diverse isocoumarins were documented and classified according to their fungal sources [16 order/28 family/55 genera] where they have been originally discovered along with their reported pharmacological activities wherever applicable. Also, recent insights around their proposed and experimentally proven biosynthetic pathways are also briefly discussed.
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