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

ABSTRACT: 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.

SUBMITTER: Schinazi RF

PROVIDER: S-EPMC8313041 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Synthesis of 2-fluoro-substituted and 2,6-modified purine 2',3'-dideoxy-2',3'-difluoro-d-arabinofuranosyl nucleosides from d-xylose.

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