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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Hongbin Sun

Volume 6, Issue 5, 2009

Page: [387 - 392] Pages: 6

DOI: 10.2174/1570180810906050387

Price: $65

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


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