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.
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.
Costache
E
E
UMR 176 CNRS-Institut Curie, Orsay, France.
Nguyen
C H
CH
Léonce
S
S
Pierré
A
A
Atassi
G
G
Bisagni
E
E
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
D000970:Antineoplastic Agents; D007211:Indoles