1-烷基-2-乙酰基-1,2,3,4-四氢异喹啉衍生物的合成及多药耐药活性(英文)

Synthesis and multidrug resistance reversal activity of 1-akyl-2-acetyl-1,2,3,4-tetrahydroisoquinoline derivatives

目的:研究脂肪酸四氢异喹啉的多药耐药活性。方法:利用Bischler-Napieralski环化反应合成一系列具有C-1长链烷基的四氢异喹啉衍生物,并以维拉帕米作为阳性对照,用MTT法进行体外细胞实验,在细胞K562和K562/DOX测定了这些化合物的肿瘤多药耐药活性。结果和结论:化合物的结构均由核磁共振氢谱,质谱,红外和元素分析确证,活性实验结果显示,化合物7,10逆转活性略低于维拉帕米,但是仍具有一定的多药耐药逆转活性。

Aim:To study the multidrug resistance activity of 1-alkyl-2-acetyl-1,2,3,4-tetrahydroisoquinoline derivatives.Methods:A series of novel tetrahydroisoquinoline derivatives bearing at C-1 position a carbon chain derived from fatty acids were prepared through the Bischler-Napieralski cyclization reaction.Their multidrug resistance(MDR)reversal cancerous multidrug resistance activities were evaluated against K562 and K562/DOX cell lines in vitro by MTT assay with verapamil as a control.Results and Conclusion:Th...