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- Title
Synthesis and antiviral evaluation of 2',3'-dideoxy- 2',3'-difluoro-D-arabinofuranosyl 2,6-disubstituted purine nucleosides.
- Authors
Schinazi, Raymond F.; Sivets, Grigorii G.; Detorio, Mervi A.; McBrayer, Tami R.; Whitaker, Tony; Coats, Steven J.; Amblard, Franck
- 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.
- Subjects
NUCLEOSIDE synthesis; ARABINOFURANOSIDASES; FURANOSIDES; PURINES; HIV infections; THERAPEUTICS; ANTIVIRAL agents; GUANOSINE derivatives
- Publication
Heterocyclic Communications, 2015, Vol 21, Issue 5, p315
- ISSN
0793-0283
- Publication type
Article
- DOI
10.1515/hc-2015-0174