Popis: |
A series of 5,11-dimethyl-6H-pyrido[3,2-b]carbazoles, structurally related to the antitumor drug ellipticine, were synthesized from 3-amino-1,4-dimethyl-9H-carbazole. Among 17 derivatives, bearing various substituents on the pyridine ring, and preliminarily evaluated for cytotoxicity on L1210-cultured cells, 13 (76%) were found to be active. One of them, 5,11-dimethyl-4-ethoxy-6H-pyrido[3,2-b]carbazole, although non-substituted on C-9, displayed an activity similar to that of 9-hydroxy-N-2-methylellipticinium acetate. Structure-activity relationships have been described in detail. |