Anti-AIDS agents-XXVIII.1 Synthesis and Anti-HIV activity of methoxy substituted 3′,4′-Di-O-(−)-camphanoyl-(+)-cis-khellactone (DCK) analogues

Four isomeric methoxy substituted DCK analogues (3–6) were asymmetrically synthesized from different starting materials. 5-Methoxy-3′,4′-di-O-(−)-camphanoyl-(+)-cis-khellactone (5) exhibited extremely potent anti-HIV activity against HIV-1 replication in H9 lymphocyte cells with EC50 and therapeutic index values of 0.00038 μM and>402,632, respectively, which are better than those of DCK and AZT in this assay.