Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors

…, GS Zhao, CG Shin, HC Zang, CK Lee, YS Lee

Index: Xu, Yu-Wen; Zhao, Gui-Sen; Shin, Cha-Gyun; Zang, Heng-Chang; Lee, Chong-Kyo; Lee, Yong Sup Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 17 p. 3589 - 3593

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Citation Number: 26

Abstract

HIV-1 integrase (IN) is an essential enzyme for retroviral replication and a rational target for the design of anti-AIDS drugs. In the present study, we have designed, synthesized and tested a series of caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors. Among these compounds, we found that HIV integrase inhibitory activities of compounds III- 3 and III-4 were more potent than l-chicoric acid (IC50= 11.8 μg/mL) and others were ...