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10,11-Dehydrocurvularin is a natural benzenediol lactone (BDL) with a 12-membered macrolide fused to a resorcinol ring produced as a secondary metabolite by many fungi. In this review, we summarized the pieces of literature regarding biosynthesis, chemical synthesis, biological activities, and assumed work mechanisms of 10,11-dehydrocurvularin, which presented a potential for agricultural and pharmaceutical uses.