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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.

par Delfourne, Evelyne;Kiss, Robert ;Le Corre, Laurent;Dujols, Frederic;Bastide, Jean;Collignon, Françoise;Lesur, Brigitte;Frydman, Armand;Darro, Francis
Référence Journal of medicinal chemistry, 46, 16, page (3536-3545)
Publication Publié, 2003-07

Article révisé par les pairs

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Résumé :

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.