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
Publication statusPublished - 1997

Fingerprint

Quinolines
Leukemia P388
Derivatives
quinoline
Lead

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Pharmacology

Cite this

Takeuchi, Y., Kitaomo, M., Chang, M. R., Shirasaka, S., Shimamura, C., Okuno, Y., ... 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.

Synthesis and antitumor activity of fused quinoline derivatives. V. Methylindolo[3,2-b]quinolines. / Takeuchi, Yasuo; Kitaomo, Masayuki; Chang, Ming Rong; Shirasaka, Shota; Shimamura, Chinami; Okuno, Yumiko; Yamato, Masatoshi; Harayama, Takashi.

In: Chemical and Pharmaceutical Bulletin, Vol. 45, No. 12, 1997, p. 2096-2099.

Research output: Contribution to journalArticle

Takeuchi, Y, Kitaomo, M, Chang, MR, 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, vol. 45, no. 12, pp. 2096-2099.
Takeuchi, Yasuo ; Kitaomo, Masayuki ; Chang, Ming Rong ; Shirasaka, Shota ; Shimamura, Chinami ; Okuno, Yumiko ; Yamato, Masatoshi ; Harayama, Takashi. / Synthesis and antitumor activity of fused quinoline derivatives. V. Methylindolo[3,2-b]quinolines. In: Chemical and Pharmaceutical Bulletin. 1997 ; Vol. 45, No. 12. pp. 2096-2099.
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