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。