Dual stimulatory and inhibitory effects of fluorine-substitution on mutagenicity: an extension of the enamine epoxide theory for activation of the quinoline nucleus

Biol Pharm Bull. 1997 Jun;20(6):646-50. doi: 10.1248/bpb.20.646.

Abstract

Nineteen mono- and di-fluorinated derivatives of quinoline, 1,7-phenanthroline, 1,10-phenanthroline, benzo[h]quinoline, and benzo[f]quinoline were subjected to analysis of their structure-mutagenicity relationships. For this purpose, six new fluorinated derivatives were synthesized. The results support that the enamine epoxide structure of the pyridine moiety, as well as the bay-region epoxide structure, is responsible for mutagenicity. Formation of K-region epoxides might involve a detoxification process rather than mutagenic activation.

Publication types

  • Comparative Study

MeSH terms

  • Benzo(a)pyrene / chemistry
  • Benzo(a)pyrene / toxicity
  • Epoxy Compounds / chemistry
  • Epoxy Compounds / toxicity*
  • Mutagenesis*
  • Mutagenicity Tests
  • Mutagens / chemistry
  • Mutagens / toxicity*
  • Phenanthrolines / chemistry
  • Phenanthrolines / toxicity
  • Quinolines / chemistry
  • Quinolines / toxicity*
  • Salmonella typhimurium / genetics
  • Structure-Activity Relationship

Substances

  • Epoxy Compounds
  • Mutagens
  • Phenanthrolines
  • Quinolines
  • Benzo(a)pyrene