海洋吡啶并吖啶生物碱海鞘胺和海鞘甲胺类似物C环和D环取代菲咯啉-7-酮衍生物的合成及其体外抗肿瘤活性

Synthesis and in vitro antitumor activity of ring C and D-substituted phenanthrolin-7-one derivatives, analogues of the marine pyridoacridine alkaloids ascididemin and meridine.

作者信息

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

机构信息

Centre de Phytopharmacie, FRE-CNRS 2605, Université de Perpignan, 52 Avenue Paul Alduy, 66860 Perpignan Cedex, France.

出版信息

Bioorg Med Chem. 2004 Aug 1;12(15):3987-94. doi: 10.1016/j.bmc.2004.06.006.

DOI:10.1016/j.bmc.2004.06.006

PMID:15246075

Abstract

A series of cycle C and D-substituted phenanthrolin-7-ones, analogues of the marine pyridoacridines meridine and ascididemin have been synthesized on the basis of Diels-Alder reactions involving quinoline-5,8-dione and 2- (or un)-substituted-N,N-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.

摘要

基于涉及喹啉-5,8-二酮与2-（或未）取代的N,N-二甲基腙的狄尔斯-阿尔德反应，合成了一系列C环和D环取代的菲咯啉-7-酮，它们是海洋吡啶并吖啶类化合物美利啶和海鞘胺的类似物。对所有化合物针对12种不同的人类癌细胞系进行了体外细胞毒性活性评估。它们均表现出细胞毒性活性，半数抑制浓度（IC50）值至少为微摩尔级别。