Synthesis and in vitro antitumor activity of an isomer of the marine pyridoacridine alkaloid ascididemin and related compounds
Synthesis and in vitro antitumor activity of an isomer of the marine pyridoacridine alkaloid ascididemin and related compounds
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DOI：
10.1016/s0968-0896(03)00483-8
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发表时间：
2003-10-01
影响因子：
3.5
通讯作者：
Darro, F
中科院分区：
文献类型：
--
作者：
Delfourne, E;Kiss, R;Darro, F
以1，4-二甲氧基吖啶（10）为原料，经六步反应合成了海鞘碱（9 H-喹啉[4，3，2-de][1，10]菲咯啉-9-酮）（1）的异构体（9 H-喹啉[4，3，2-de][1，7]菲咯啉-9-酮）（2），总收率12%。制备了不同的相关化合物，并在不同组织病理学类型（胶质母细胞瘤和乳腺癌、结肠癌、肺癌、前列腺癌和膀胱癌）的12种不同人类癌细胞系上以6种不同浓度进行体外测试。几乎所有的化合物都具有微摩尔级的细胞毒活性。(C)2003爱思唯尔有限公司。保留所有权利。
The isomer (9H-quino[4,3,2-de][1,7]phenanthroline-9-one) (2) of the marine alkaloid ascididemin (9H-quino[4,3,2-de][1,10]phenanthroline-9-one) (1) has been synthesized in six steps from 1,4-dimethoxyacridine (10) with an overall yield of 12%. Different related compounds were prepared and tested in vitro at six different concentrations on 12 different human cancer cell lines of various histopathological types (glioblastomas and breast, colon, lung, prostate and bladder cancers). Almost all the Compounds present cytotoxic activity of micromolar order. (C) 2003 Elsevier Ltd. All rights reserved.