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

Autor: Steven J. Coats, Grigorii G. Sivets, Tami R. McBrayer, Mervi Detorio, Tony Whitaker, Raymond F. Schinazi, Franck Amblard
Rok vydání: 2021
Předmět:
Zdroj: Heterocycl Comm
ISSN: 0793-0283
Popis: 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.
Databáze: OpenAIRE