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

Heterocycl Comm

Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA; and Veterans Affairs Medical Center, Decatur, GA 30033, USA.

Published: October 2015

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 and guanosine derivative demonstrate potent anti-HIV-1 activity (EC = 0.56 and 0.65 μM; EC = 4.2 and 3.1 μM) while displaying only moderate cytotoxicity in primary human lymphocytes.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8313041PMC
http://dx.doi.org/10.1515/hc-2015-0174DOI Listing

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