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

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

Journal Name: Letters in Drug Design & Discovery

Volume 6 , Issue 5 , 2009

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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

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Article Details

Year: 2009
Page: [387 - 392]
Pages: 6
DOI: 10.2174/1570180810906050387
Price: $65

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