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

2',3'-二脱氧-2',3'-二氟-D-阿拉伯呋喃糖基2,6-二取代嘌呤核苷的合成及抗病毒活性评价

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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 (EC(50) = 0.56 and 0.65 μM; EC(90) = 4.2 and 3.1 μM) while displaying only moderate cytotoxicity in primary human lymphocytes.

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