Silyl modification of biologically active compounds. 13. Synthesis, cytotoxicity and antibacterial action of<i>N</i>-methyl-<i>N</i>-(2-triorganylsiloxyethyl)-1,2,3,4-tetrahydro(iso)quinolinium iodides
作者:Alla Zablotskaya、Izolda Segal、Yuris Popelis、Solveiga Grinberga、Irina Shestakova、Vizma Nikolajeva、Daina Eze
DOI:10.1002/aoc.2952
日期:2013.2
A series of N‐methyl‐N‐(2‐triorganylsiloxyethyl)‐1,2,3,4‐tetrahydro(iso)quinolinium iodides has been synthesized via dehydrocondensation reaction of N‐(2‐hydroxyethyl)‐1,2,3,4‐tetrahydroisoquinoline, N‐(2‐hydroxyethyl)‐1,2,3,4‐tetrahydroquinoline and 4,4‐dimethyl‐N‐(2‐hydroxyethyl)‐4‐sila‐1,2,3,4‐tetrahydroisoquinoline with trialkyl(aryl)hydrosilanes and subsequent alkylation, and characterized by
通过N-(2-羟乙基)-1,2,3的脱氢反应合成了一系列N-甲基-N-(2-三有机基甲硅烷氧基乙基)-1,2,3,4-四氢(异)喹啉碘化物。 4-四氢异喹啉,N-(2-羟乙基)-1,2,3,4-四氢喹啉和4,4-二甲基-N-(2-羟乙基)-4-sila-1,2,3,4-四氢异喹啉三烷基(芳基)氢硅烷和随后的烷基化反应,其特征在于1 H,13 C和29Si NMR和质谱。与2-羟乙基前体相比,生物学活性数据显示出对肿瘤细胞系和几乎所有测试细菌/真菌菌株的抑制活性显着增强。大多数化合物对HT‐1080(人纤维肉瘤)和MG‐22A(小鼠肝癌)癌细胞系的细胞毒性都在微克范围内。版权所有©2012 John Wiley&Sons,Ltd.