Phosphorylation, anti-HIV activity and cytotoxicity of 3'-fluorothymidine |
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Authors: | E Matthes C Lehmann D Scholz H A Rosenthal P Langen |
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Institution: | Central Institute of Molecular Biology, Academy of Sciences, GDR, Berlin-Buch. |
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Abstract: | 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. |
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