Anti-AIDS agents. Part 58: Synthesis and anti-HIV activity of 1-thia-di-O-(−)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues ☆

Abstract Two 1-thia-DCK analogues ( 9a and 9b ) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 9a showed excellent anti-HIV activity with an EC 50 value of 0.00012 μM and therapeutic index of 1,408,000. Compound 9b was less active with EC 50 and TI values of 3.11 μM and 62.3, respectively. The bioassay results indicated that thia-DCK analogues merit attention as potential HIV-1 inhibitors.