Add time:08/29/2019         Source:sciencedirect.com

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.

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