title: Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors.
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 (IC(50)=11.8 microg/mL) and others were comparable to L-chicoric acid. Furthermore, the structure-activity relationships of these compounds were studied. The information gathered from this paper will be useful in the development and design of HIV-1 integrase inhibitors in the future.
authors.affiliation: College of Pharmacy, Shandong University, PO Box 111, 44# Wenhuaxi Road, Ji'nan 250012, Shandong Province, PR China.
authors.forename: Yu-Wen
authors.initials: YW
authors.lastname: Xu
authors.forename: Gui-Sen
authors.initials: GS
authors.lastname: Zhao
authors.forename: Cha-Gyun
authors.initials: CG
authors.lastname: Shin
authors.forename: Heng-Chang
authors.initials: HC
authors.lastname: Zang
authors.forename: Chong-Kyo
authors.initials: CK
authors.lastname: Lee
authors.forename: Yong Sup
authors.initials: YS
authors.lastname: Lee
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D019427:HIV Integrase / Q000737:chemistry / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D019428:HIV Integrase Inhibitors; D013449:Sulfonamides; C051353:naphthalenesulfonamide; D019427:HIV Integrase