Potent antiviral 2′-fluoro-arabinosyl pyrimidine nucleosides: lack of mutagenic activity

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Abstract
The carcinogenicity of many drugs, such as antitumor agents, is a subject of growing concern. The newly developed pyrimidine nucleosides, 2''-fluoro-5-iodo-1-.beta.-D-arabinofuranosylcytosine (FIAC) and 2''-fluoro-1-.beta.-D-arabinofuranosyl-5-methyluracil (FMAU), show potent anti-herpes virus activity in tissue cultures, laboratory animals and man, and an activity to inhibit the growth of certain tumor cell lines in vitro. Radioactivity of 14C-labeled FIAC and FMAU is incorporated into the DNA of normal and neoplastic mammalian tissues. FIAC and FMAU are inactive in a bacterial mutagenesis assay (Salmonella-microsome test) and in a mammalian cell mutagenesis assay employing V79 Chinese hamster cells in vitro. Both agents did not induce unscheduled DNA synthesis in primary Wistar rat hepatocytes in vitro.