Selective inhibition of human immunodeficiency virus (HIV) by 3'-azido-2', 3'-dideoxyguanosine in vitro

3'-Azido-2',3'-dideoxyguanosine (AzddGuo) is a potent and selective inhibitor of human immunodeficiency virus (HIV) in vitro. AzddGuo completely inhibits HIV-induced cytopathogenicity and viral antigen expression in MT-4 cells at a concentration of 5.0 microM. Its 50% effective dose for inhibiting HIV-induced cytopathogenicity is 1.4 microM, as compared to 6.4 microM for 2',3'-dideoxyadenosine (ddAdo). Thus, AzddGuo is approximately 4.6-fold more potent as an anti-HIV agent than ddAdo, one of the most promising compounds for the treatment of AIDS. However, AzddGuo is about 4.7 times more cytotoxic than ddAdo, so that its selectivity index, as based on the ratio of the 50% cytotoxic dose to the 50% antiviral effective dose, is almost the same as that of ddAdo (136 and 139, respectively).