In vitro cytotoxicity of carbazole derivatives IV. 5.11-Dimethyl-6H-pyridocarbazoles substituted on the pyridine ring

Article abstract of DOI:10.1016/0223-5234(93)90032-A

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 (76percent) 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-methyl-ellipticinium acetate.Structure-activity relationships have been described in detail. cytotoxicity/leukemia L1210/clonogenic assay/pyrido<3,2-b>carbazoles