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XUE Ling-jing, MIN Tao, SUN Min-jie, ZHANG Can, SUN Hong-bin. Synthesis and multidrug resistance reversal activity of 1-akyl-2-acetyl-1，2，3，4-tetrahydroisoquinoline derivatives[J]. Journal of China Pharmaceutical University, 2009, 40(5): 389-394.
Citation: XUE Ling-jing, MIN Tao, SUN Min-jie, ZHANG Can, SUN Hong-bin. Synthesis and multidrug resistance reversal activity of 1-akyl-2-acetyl-1，2，3，4-tetrahydroisoquinoline derivatives[J]. Journal of China Pharmaceutical University, 2009, 40(5): 389-394.
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Synthesis and multidrug resistance reversal activity of 1-akyl-2-acetyl-1，2，3，4-tetrahydroisoquinoline derivatives

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  • 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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