Synthesis and antitumor activity of fused quinoline derivatives. V. Methylindolo[3,2-b]quinolines.
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.
Takeuchi
Y
Y
Faculty of Pharmaceutical Sciences, Okayama University, Japan.
Kitaomo
M
M
Chang
M R
MR
Shirasaka
S
S
Shimamura
C
C
Okuno
Y
Y
Yamato
M
M
Harayama
T
T
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D007941:Leukemia P388 / Q000188:drug therapy*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D007211:Indoles; D011804:Quinolines