Design, synthesis and molecular modeling of aloe-emodin derivatives as potent xanthine oxidase inhibitors

DH Shi, W Huang, C Li, YW Liu, SF Wang

Index: Shi, Da-Hua; Huang, Wei; Li, Chao; Liu, Yu-Wei; Wang, Shi-Fan European Journal of Medicinal Chemistry, 2014 , vol. 75, p. 289 - 296

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Citation Number: 7

Abstract

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 ...