Antitumour polycyclic acridines. Part 10.1 Synthesis of penta- and hexa-cyclic heteroaromatic systems by radical cyclisations of substituted 9-anilinoacridines
作者:Michael J. Ellis、Malcolm F. G. Stevens
DOI:10.1039/b106327h
日期:2001.11.29
9-Anilinoacridines substituted with a bromine atom in the 2-position of the anilino group or the 1-position of the acridine moiety can be cyclised with tributyltin hydride–AIBN to penta- or hexacyclic acridines. Of the polycyclic systems 13,14-dihydropyrrolo[3′,2′,1′:8,1]quino[4,3,2-kl]acridine 14a is the most potent cytotoxic agent displaying a mean GI50 concentration against a panel of 60 human tumour
在其2位上被溴原子取代的9-苯胺基idine啶 安尼利诺集团 或the啶部分的1位可以用 氢化三丁基锡–AIBN为五环或六环 啶。在多环体系中13,14-dihydropyrrolo [3',2',1':8,1] quino [4,3,2- kl ] ac啶14a是最有效的细胞毒性剂,相对于检测组显示平均GI 50浓度0.06μM的60种人类肿瘤细胞系中