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  • 标题:Dual Stimulatory and Inhibitory Effects of Fluorine-Substitution on Mutagenicity : An Extension of the Enamine Epoxide Theory for Axtivation of the Quinoline Nucleus
  • 本地全文:下载
  • 作者:Ken-ichi SAEKI ; Hiroshi KAWAI ; Yutaka KAWAZOE
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1997
  • 卷号:20
  • 期号:6
  • 页码:646-650
  • DOI:10.1248/bpb.20.646
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要: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.
  • 关键词:quinoline;fluoroquinoline;mutagenicity;metabolism;benzoquinoline;phenanthroline
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