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）

薛玲静; 闵涛; 孙敏捷; 张灿; 孙宏斌

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

摘要

摘要: 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。

Abstract: 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 ：The structures of these tetrahydroisoquinolines were confirmed by extensive spectroscopic methods(¹H NMR，MS，IR and elemental analyses).MDR results showed that compounds 7 and 10 exhibited moderate reversal activities，and were slightly less potent than those of verapamil against K562 cell line.It is believed that compounds 7 and 10 have MDR activity.}}

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