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Synthesis and Anti-HIV Integrase Inhibitory Activity of β-Diketo Derivatives of Mono-Substituted Calix[4]arene

Six β-diketo derivatives of mono-substituted calix[4]arene were synthesized as potential HIV-1 integrase inhibitors and evaluated their inhibition to the strand transfer process of HIV-1 integrase. Their structures were characterized by NMR and HRMS. All the title compounds as potential HIV-1 integrase inhibitors proved to be active in the micromolar range (6.7–37.6 μM) on the strand transfer step.