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

摘要

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.