Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications

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Abstract
New modifications of 10-[[3-(diethylamino)propyl]amino]-6-methyl-5H-pyrido[3'',4'':4,5]pyrrolo[2,3-g]isoquinoline (1b) and 1-[[3-(diethylamino)propyl]amino]-9-methoxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazole (4b), which display important antitumor properties, were performed on the side chain or on the intercalating heterocycle. Side chains were introduced by direct substitution of the corresponding chloro derivatives; 6-N-methyl-9-hydroxypyrido[4,3-b]carbazoles analogs were prepared via 9-O-benzoyl-1-chloroellipyticines. Evaluation of all new compounds shows no significant increase of in vitro cytotoxicity and percent ILS [increase in life span] on the L1210 [mouse] leukemia system by comparison with the model compounds 1b and 4b.