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

Abstract 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 EC 50 and therapeutic index values of −7 μM and >3.72 × 10 8 , respectively, which are much better than those of DCK and AZT in this assay.