Anti-AIDS agents. Part 56: Synthesis and anti-HIV activity of 7-thia-di-O-(−)-camphanoyl-(+)-cis-khellactone (7-thia-DCK) analogs

Abstract Two thia-DCK analogs ( 3a , b ) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 3a showed potent anti-HIV activity with an EC 50 value of 0.14 μM and a therapeutic index of 1110. However, the corresponding 6- tert -butyl-substituted compound ( 3b ) showed no suppression. The bioassay results indicated that thia-DCK analogs merit attention as potential HIV-1 inhibitors.