Abstract A series of aloe-emodin derivatives were synthesized and evaluated as xanthine oxidase inhibitors. Among them, four aloe-emodin derivatives showed significant inhibitory activities against xanthine oxidase. The compound 4, 5-dihydroxy-9, 10-dioxo-9, 10- dihydroanthracene-2-carbaldehyde (A1) possessed the best xanthine oxidase inhibitory activity with IC 50 of 2.79 μM. Lineweaver–Burk plot analysis revealed that A1 acted as a ...