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
Letters in Drug Design & Discovery
Title: 1-Benzyl-1,2,3,4-tetrahydroisoquinoline Derivatives and Optically Pure Isomers as Novel Promising Multidrug Resistance (MDR) Reversing Agents
Volume: 6 Issue: 5
Author(s): Lingjing Xue, Minjie Sun, Tao Min, Can Zhang and Hongbin Sun
Affiliation:
Keywords: Tetrahydroisoquinoline, Optical pure isomers, Multidrug resistance, P-glycoprotein, Synthesis, Reversing agents
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.
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Cite this article as:
Xue Lingjing, Sun Minjie, Min Tao, Zhang Can and Sun Hongbin, 1-Benzyl-1,2,3,4-tetrahydroisoquinoline Derivatives and Optically Pure Isomers as Novel Promising Multidrug Resistance (MDR) Reversing Agents, Letters in Drug Design & Discovery 2009; 6 (5) . https://dx.doi.org/10.2174/1570180810906050387
DOI https://dx.doi.org/10.2174/1570180810906050387 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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