DNA intercalating compounds as potential antitumor agents. 1. Preparation and properties of 7H-pyridocarbazoles

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Abstract
The DNA intercalating compounds derived from 6H-pyridocarbazole (ellipticines, olivacines) elicit high antitumor properties. To get information about the mechanism of action of these agents it is necessary to study structurally related analogs. For this purpose, various derivatives of the 4 isomeric 7H-pyridocarbazoles were synthesized by a single photochemical process on indolylpyridylethylenes. These derivatives are able to intercalate into DNA. The DNA binding affinities vary in the range of 104 to 106 M-1, depending mainly on the nature of the substituent, N quaternization being the most enhancing factor. The position of the pyridinic N does not markedly affect the DNA binding affinity. Three quaternized compounds elicit a significative but low antileukemic activity on L1210 mice leukemia cells. The properties of 7H-pyridocarbazoles are discussed and compared to those of 6H-pyridocarbazoles (ellipticines and olivacines).

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