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

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.