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

  • H Marquardt
  • Johannes Westendorf

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), have shown 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. However, we now report that 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.

Bibliographical data

Original languageGerman
Article number5
ISSN0143-3334
Publication statusPublished - 1982
pubmed 7046983