Pyrrolo-quinoline derivatives as potential antineoplastic drugs

Some novel pyrrolo-quinoline derivatives have been synthesized as potential antineoplastic agents. They contain an angular aromatic tricyclic or tetra cyclic system, to which the methanesulfon-anisidide side chain typical of a msacrine as such, or lacking the m-methoxy substituent, is connected. A met hyl group can be present at position 7 of the pyrrolo-quinoline ring. The n ovel compounds exhibit interesting cell growth inhibitory properties when t ested against the NCI panel of cell lines, in particular those obtained fro m solid tumors like CNS-, melanoma- and prostate-derived cells. The mechani sm of cytotoxic action does not seem to be related to topoisomerase II pois oning ability. Most active proved to be compound 4a, which lacks both methy l and methoxy substituents, followed by 5a, having the methoxy group only. Biological activity is less pronounced in the tetracyclic family of derivat ives 6 and 7. (C) 2000 Elsevier Science Ltd. All rights reserved.