The chemical constituents produced by Chinese higher fungi, including thirty two basidiomycete and six ascomycete species, have been investigated in the past decades. A variety of new secondary metabolites associated with diverse structural types of terpenoids, steroids, sphingolipids, perylenequinones, p-terphenyls, pyranones, and heterocyclic compounds, which exhibited antitumor, anti-inflammatory, cytotoxic, enzyme inhibitory, antiviral, neuritogenic, antibiotic, and other activities, have been discovered. Recent progress in the structures and interesting biological properties of compounds isolated from these higher fungi is discussed in this review.