Synthesis and cytotoxic evaluation of analogues of the marine pyridoacridine amphimedine
作者:Christine Brahic、Francis Darro、Mirabelle Belloir、Jean Bastide、Robert Kiss、Evelyne Delfourne
DOI:10.1016/s0968-0896(02)00148-7
日期:2002.9
2-de][1,8] or [1,9]-phenanthroline-7-ones and 9-methyl-1,4-diazanaphtacene-3,10-dione, analogues of the marine pyridoacridine amphimedine were synthesised from isoquinoline-5,8-dione. The first compounds were obtained starting from a Diels-Alder reaction whereas the synthesis of the last compound was initiated by a reaction of condensation with 2-aminoacetophenone. The different tetra- and pentacyclic
4-取代的7H-吡啶基-[4,3,2-de] [1,8]或[1,9]-菲咯啉-7-ones和9-methyl-1,4-diazanaphtacene-3,10-dione ,从异喹啉-5,8-二酮合成海洋吡啶并ido啶两性霉素的类似物。从Diels-Alder反应开始获得第一种化合物,而最后一种化合物的合成通过与2-氨基苯乙酮缩合的反应而开始。评价了不同的四环和五环化合物对六种不同的人类癌细胞系的体外细胞毒性活性。所有化合物均显示出具有IC(50)值的细胞毒性活性(即,其中两种药物浓度抑制六个细胞系的平均生长值50%)<10(-7)M。