title: 1-Amino-substituted 8-hydroxy-4,5-dimethyl-5H-pyrido[4,3-b]indoles with propyl- or methyl substituents at the 9-, and 7,9-positions: synthesis and biological evaluation.
abstract: The title compounds were synthesized in 9-10 steps in order to compare their cytotoxic properties to that for 1-(3-dimethylaminopropyl)-amino-4,5-dimethyl- 8-hydroxy-5H-pyrido[4,3-b]indole. Whereas the latter is a potent cytotoxic agent, displaying significant antitumour activity, the corresponding 9-propyl (and 7,9-dimethyl) derivatives were found to be > 10-fold less cytotoxic.
authors.affiliation: UMR 176 CNRS-Institut Curie, Orsay, France.
authors.forename: E
authors.initials: E
authors.lastname: Costache
authors.forename: C H
authors.initials: CH
authors.lastname: Nguyen
authors.forename: S
authors.initials: S
authors.lastname: Léonce
authors.forename: A
authors.initials: A
authors.lastname: Pierré
authors.forename: G
authors.initials: G
authors.lastname: Atassi
authors.forename: E
authors.initials: E
authors.lastname: Bisagni
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles