Delfourne Evelyne, Kiss Robert, Le Corre Laurent, Dujols Frederic, Bastide Jean, Collignon Françoise, Lesur Brigitte, Frydman Armand, Darro Francis
Centre de Phytopharmacie, UMR-CNRS 5054, Université de Perpignan, 52 Avenue de Villeneuve, 66860 Perpignan Cedex, France.
J Med Chem. 2003 Jul 31;46(16):3536-45. doi: 10.1021/jm0308702.
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.
一系列取代的吡啶并[4,3,2 - de][1,7]或[1,10] - 菲咯啉 - 7 - 酮，即海洋吡啶吖啶类化合物美利啶和海鞘素的类似物，已基于涉及不同喹啉 - 5,8 - 二酮和N,N - 醛基二甲基腙的狄尔斯 - 阿尔德反应合成。对所有化合物进行了针对12种不同人类癌细胞系的体外细胞毒性活性评估。它们均表现出细胞毒性活性，IC(50)值至少为微摩尔级。
