Phosphorylation, anti-HIV activity and cytotoxicit...[Biochem Biophys Res Commun. 1988]

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1: Biochem Biophys Res Commun. 1988 Jun 16;153(2):825-31. Links

Phosphorylation, anti-HIV activity and cytotoxicity of 3'-fluorothymidine.

Matthes E, Lehmann C, Scholz D, Rosenthal HA, Langen P.

Central Institute of Molecular Biology, Academy of Sciences, GDR, Berlin-Buch.

3'-fluorothymidine (FddThd) is well phosphorylated to the 5'-triphosphate in various relevant cell-lines. This results in fairly stable levels of this compound without accumulation of the 5'-monophosphate to the extent described for 3'-azidothymidine (AzT). The di- and triphosphate of FddThd seems unable to influence the ribonucleotide reductase in permeable cells. FddThd protects 50% of the MT-4 cells against the cytopathic effect of HIV at 3 nM, but reduces the number of uninfected viable cells to 50% at 1.1 microM. All other tested human cell-lines displayed a far less antiproliferative sensitivity to FddThd, comparable with that of AzT.

PMID: 3164184 [PubMed - indexed for MEDLINE]

Phosphorylation of 3'-azido-3'-deoxythymidine and selective interaction of the 5'-triphosphate with human immunodeficiency virus reverse transcriptase. [Proc Natl Acad Sci U S A. 1986]
Both 2',3'-dideoxythymidine and its 2',3'-unsaturated derivative (2',3'-dideoxythymidinene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro. [Biochem Biophys Res Commun. 1987]
Differential patterns of intracellular metabolism of 2',3'-didehydro-2',3'-dideoxythymidine and 3'-azido-2',3'-dideoxythymidine, two potent anti-human immunodeficiency virus compounds. [J Biol Chem. 1989]
ReviewSpectrum of antiviral activity and mechanism of action of zidovudine. An overview. [Am J Med. 1988]
ReviewSulfated polysaccharides extracted from sea algae as potential antiviral drugs. [Gen Pharmacol. 1997]

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Phosphorylation, anti-HIV activity and cytotoxicity of 3'-fluorothymidine.

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