Synthesis and multidrug resistance reversal activity of 1-akyl-2-acetyl-1,2,3, 4-tetrahydroisoquinoline derivatives / 中国药科大学学报

ABSTRACT

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 ana-lyses). 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.