Delfourne Evelyne, Kiss Robert, Le Corre Laurent, Merza Joumaa, Bastide Jean, Frydman Armand, Darro Francis
Centre de Phytopharmacie, FRE-CNRS 2605, Université de Perpignan, 52 Avenue de Villeneuve, 66860 Perpignan, France.
Bioorg Med Chem. 2003 Oct 1;11(20):4351-6. doi: 10.1016/s0968-0896(03)00483-8.
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.
海洋生物碱海鞘胺(9H-喹啉并[4,3,2-de][1,10]菲咯啉-9-酮)(1)的异构体(9H-喹啉并[4,3,2-de][1,7]菲咯啉-9-酮)(2)已由1,4-二甲氧基吖啶(10)经六步合成,总产率为12%。制备了不同的相关化合物,并在体外对六种不同浓度的12种不同组织病理学类型的人类癌细胞系(胶质母细胞瘤以及乳腺癌、结肠癌、肺癌、前列腺癌和膀胱癌)进行了测试。几乎所有化合物都具有微摩尔级的细胞毒性活性。