Synthesis and cytotoxic evaluation of analogues of the marine pyridoacridine amphimedine
Synthesis and cytotoxic evaluation of analogues of the marine pyridoacridine amphimedine
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DOI：
10.1016/s0968-0896(02)00148-7
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发表时间：
2002-09-01
影响因子：
3.5
通讯作者：
Delfourne, E
中科院分区：
文献类型：
--
作者：
Brahic, C;Darro, F;Delfourne, E
4-取代-7H-吡啶-[4，3.2-de][1，8]或[1，9]-菲咯啉-7-酮和9-甲基-1，4-二氮杂二茂-3，10-二酮。以异喹啉-5，8-二酮为原料合成了海洋吡喃并苯并咪啶的类似物。第一个化合物是从Diels-Alder反应开始的，而最后一个化合物的合成是通过与2-氨基苯乙酮的缩合反应开始的。不同的四环和五环化合物在体外对6个不同的人类癌细胞株具有细胞毒活性。所有化合物都具有细胞毒活性，其中两个化合物的IC50值(即药物浓度对六种细胞株的平均生长抑制50%)<；10(-7)M。(C)2002爱思唯尔科学有限公司。保留所有权利。
4-Substituted-7H-pyrido-[4,3.2-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 compounds were evaluated for in vitro cytotoxic activities against six distinct human cancer cell lines. All the compounds exhibit cytotoxic activity with IC50 values (i.e., the drug concentration inhibiting the mean growth value of the six cell lines by 50%) < 10(-7) M for two of them. (C) 2002 Elsevier Science Ltd. All rights reserved.