Anti-aids agents 33.1 Synthesis and anti-HIV activity of mono-methyl substituted 3′,4′-di-O-(−)-camphanoyl-(+)-cis-khellactone (DCK) analogues

Four isomeric methyl substituted DCK analogues (2–5) were asymmetrically synthesized from different starting materials. 3-Methyl, 4-methyl, and 5-methyl-3′,4′-di-O-(−)-camphanoyl-(+)-cis-khellactone (2–4) all were extremely potent against HIV-1 replication in H9 lymphocyte cells with EC50 and therapeutic index values of <4.23 × 10−7 μM and >3.72 × 108, respectively, which are much better than those of DCK and AZT in this assay.