Synthesis and antiviral evaluation of 2',3'-dideoxy- 2',3'-difluoro-D-arabinofuranosyl 2,6-disubstituted purine nucleosides.

The synthesis of new 2,6-disubstituted purine 2',3'-dideoxy-2',3'-difluoro-D-arabino nucleosides is reported. Their ability to block HIV and HCV replication along with their cytotoxicity toward Huh-7 cells, human lymphocyte, CEM and Vero cells was also assessed. Among them, β-2,6-diaminopurine nucleoside 25 and guanosine derivative 27 demonstrate potent anti-HIV-1 activity (EC₅₀ = 0.56 and 0.65 µm; EC₉₀ = 4.2 and 3.1 µm) while displaying only moderate cytotoxicity in primary human lymphocytes. [ABSTRACT FROM AUTHOR]