Chemical and Pharmaceutical Bulletin p. 2096 - 2099 (1997)
Update date:2022-08-06
Topics:
Takeuchi, Yasuo
Kitaomo, Masayuki
Chang, Ming-Rong
Shirasaka, Shota
Shimamura, Chinami
Okuno, Yumiko
Yamato, Masatoshi
Harayama, Takashi
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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