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

doi:10.1248/cpb.45.2096

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 journal › Article › peer-review

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 language	English
Pages (from-to)	2096-2099
Number of pages	4
Journal	Chemical and Pharmaceutical Bulletin
Volume	45
Issue number	12
DOIs	https://doi.org/10.1248/cpb.45.2096
Publication status	Published - 1997

Keywords

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

ASJC Scopus subject areas

Chemistry(all)
Drug Discovery

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10.1248/cpb.45.2096

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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.",

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author = "Yasuo Takeuchi and Masayuki Kitaomo and Chang, {Ming Rong} and Shota Shirasaka and Chinami Shimamura and Yumiko Okuno and Masatoshi Yamato and Takashi Harayama",

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T1 - Synthesis and antitumor activity of fused quinoline derivatives. V. Methylindolo[3,2-b]quinolines

AU - Takeuchi, Yasuo

AU - Kitaomo, Masayuki

AU - Chang, Ming Rong

AU - Shirasaka, Shota

AU - Shimamura, Chinami

AU - Okuno, Yumiko

AU - Yamato, Masatoshi

AU - Harayama, Takashi

PY - 1997

Y1 - 1997

N2 - 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.

AB - 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.

KW - Antitumor activity

KW - Indolol[3,2-b]quinoline

KW - Structure-activity relationship

KW - Synthesis

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

Abstract

Keywords

ASJC Scopus subject areas

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