Synthesis and antitumor activity of fused quinoline derivatives. V. Methylindolo[3,2-b]quinolines

Yasuo Takeuchi, Masayuki Kitaomo, Ming Rong Chang, Shota Shirasaka, Chinami Shimamura, Yumiko Okuno, Masatoshi Yamato, Takashi Harayama

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

Indolo[3,2-b]quinoline derivatives (1b-i) with a methyl group at each possible position have been synthesized. The 1-methyl (1b) and 9-methyl (1i) derivatives were inactive, but the 3-methyl (1d), 4-methyl (1e), and 6- methyl (1f) derivatives exhibited high treatment/control (T/C) value and cure rates against leukemia P388 in mice. These results indicated that modification of indolo[3,2-b]quinoline derivatives at 3, 4, and 6 positions may be useful approach for lead optimization.

Original languageEnglish
Pages (from-to)2096-2099
Number of pages4
JournalChemical and Pharmaceutical Bulletin
Volume45
Issue number12
DOIs
Publication statusPublished - Jan 1 1997

Keywords

  • Antitumor activity
  • Indolol[3,2-b]quinoline
  • Structure-activity relationship
  • Synthesis

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

Fingerprint Dive into the research topics of 'Synthesis and antitumor activity of fused quinoline derivatives. V. Methylindolo[3,2-b]quinolines'. Together they form a unique fingerprint.

  • Cite this

    Takeuchi, Y., Kitaomo, M., Chang, M. R., Shirasaka, S., Shimamura, C., Okuno, Y., Yamato, M., & Harayama, T. (1997). Synthesis and antitumor activity of fused quinoline derivatives. V. Methylindolo[3,2-b]quinolines. Chemical and Pharmaceutical Bulletin, 45(12), 2096-2099. https://doi.org/10.1248/cpb.45.2096