Synthesis and Antitumor Activity of Fused Quinoline Derivatives

Masatoshi Yamato, Yasuo Takeuchi, Ming rong Chang, Kuniko Hashigaki, Takashi Tsuruo, Tazuko Tashiro, Shigeru Tsukagoshi

Research output: Contribution to journalArticlepeer-review

33 Citations (Scopus)


Some tetracyclic quinolines (9 and 14) with a [2-methoxy-4-[(methylsulfonyl)amino]phenyl]amino side chain were prepared and their deoxyribonucleic acid (DNA) intercalative properties, KB cytotoxicity, antitumor activity (P388 leukemia), and ability to induce topoisomerase II dependent DNA cleavage were investigated. The indoloquinoline derivative 9 exhibited the most potent activity (dose = 6.3 mg, T/C% = 300) in this series. The steric structural features of the chromophores of the compounds previously and newly synthesized were studied by a computer-associated molecular graphics technique. Relationships between the steric structural features of the chromophores and biological activities are also discussed.

Original languageEnglish
Pages (from-to)3048-3052
Number of pages5
JournalChemical and Pharmaceutical Bulletin
Issue number11
Publication statusPublished - 1990


  • antitumor activity
  • indoloquinoline
  • intercalation
  • molecular graphics
  • synthesis
  • topoisomerase II

ASJC Scopus subject areas

  • General Chemistry
  • Drug Discovery


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