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Synthesis and in Vitro Antitumor Activity of Phenanthrolin-7-one Derivatives, Analogues of the Marine Pyridoacridine Alkaloids Ascididemin and Meridine: Structure−Activity Relationship

2003; American Chemical Society; Volume: 46; Issue: 16 Linguagem: Inglês

10.1021/jm0308702

1520-4804

Evelyne Delfourne, Róbert Kiss, Laurent Le Corre, Frédéric Dujols, Jean Bastide, Françoise Collignon, Brigitte Lesur, Armand Frydman, Francis Darro,

Marine Sponges and Natural Products

A series of substituted pyrido[4,3,2-de][1,7] or [1,10]-phenanthrolin-7-ones, analogues of the marine pyridoacridines meridine and ascididemin, have been synthesized on the basis of Diels-Alder reactions involving different quinoline-5,8-diones and N,N-aldehyde-dimethylhydrazones. All the compounds were evaluated for in vitro cytotoxic activity against 12 distinct human cancer cell lines. They all exhibit cytotoxic activity with IC(50) values at least of micromolar order.