Saeki K, Kawai H, Kawazoe Y, Hakura A
Faculty of Pharmaceutical Sciences, Nagoya City University, Japan.
Biol Pharm Bull. 1997 Jun;20(6):646-50. doi: 10.1248/bpb.20.646.
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.
对喹啉、1,7-菲咯啉、1,10-菲咯啉、苯并[h]喹啉和苯并[f]喹啉的19种单氟和二氟衍生物进行了结构-致突变性关系分析。为此，合成了6种新的氟化衍生物。结果表明，吡啶部分的烯胺环氧化物结构以及湾区环氧化物结构是致突变性的原因。K区环氧化物的形成可能涉及解毒过程而非诱变激活。
