Anti-HIV-1 activities of 1,3-dioxolane guanine and 2,6-diaminopurine dioxolane.
DXG and its prodrug DAPD have been demonstrated to be effective inhibitors of HIV-1 in various cells. The EC50s for DXG were 0.032 microM in CBMCs and 0.05 microM in MT-4 cells, which were generally equipotent as 3TC. 3TC-resistant, but not AZT-resistant, HIV-1 had minimum diminished sensitivity to the compounds. Both DXG and DAPD were non-toxic to cells up to 500 microM.
Gu
Z
Z
BioChem Therapeutics Inc., Laval, Quebec, Canada.
Wainberg
M A
MA
Nguyen-Ba
P
P
L'Heureux
L
L
de Muys
J M
JM
Rando
R F
RF
D019380:Anti-HIV Agents / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D004148:Dioxolanes / Q000494:pharmacology*; D004352:Drug Resistance, Microbial; D006151:Guanosine / Q000031:analogs & derivatives* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D011684:Purine Nucleosides / Q000494:pharmacology*
D019380:Anti-HIV Agents; D004148:Dioxolanes; D011684:Purine Nucleosides; C098394:dioxolane guanosine; D006151:Guanosine; C098393:amdoxovir