title: Synthesis and antitumor activity of fused quinoline derivatives. V. Methylindolo[3,2-b]quinolines.
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.
authors.affiliation: Faculty of Pharmaceutical Sciences, Okayama University, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Takeuchi
authors.forename: M
authors.initials: M
authors.lastname: Kitaomo
authors.forename: M R
authors.initials: MR
authors.lastname: Chang
authors.forename: S
authors.initials: S
authors.lastname: Shirasaka
authors.forename: C
authors.initials: C
authors.lastname: Shimamura
authors.forename: Y
authors.initials: Y
authors.lastname: Okuno
authors.forename: M
authors.initials: M
authors.lastname: Yamato
authors.forename: T
authors.initials: T
authors.lastname: Harayama
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D011804:Quinolines