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

Article abstract of DOI:10.1016/S0960-894X(98)00367-9

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 x 10^-7 μM and >3.72 x 10⁸, respectively, which are much better than those of DCK and AZT in this assay.