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Letters in Drug Design & Discovery

Author(s): Lingjing Xue, Minjie Sun, Tao Min, Can Zhang and Hongbin Sun

DOI: 10.2174/1570180810906050387

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1-Benzyl-1,2,3,4-tetrahydroisoquinoline Derivatives and Optically Pure Isomers as Novel Promising Multidrug Resistance (MDR) Reversing Agents

Page: [387 - 392] Pages: 6

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Abstract

A series of chiral compounds were designed and synthesized as novel multidrug resistance (MDR) modulators on the basis of tetrahydroisoquinolines to reverse cancerous MDR on K562 cells and K562/DOX cells by using the MTT assay. The treatment of K562/DOX cells with 9e, 10a and 10e led to increased intracellular accumulation and decreased efflux of doxorubicin. The pharmacological effects of these tetrahydroisoquinolines on P-glycoprotein (P-gp) mediated MDR were much stronger than that of positive control drug verapamil.

Keywords: Tetrahydroisoquinoline, Optical pure isomers, Multidrug resistance, P-glycoprotein, Synthesis, Reversing agents