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Partial synthesis and biological evaluation of bisbenzylisoquinoline alkaloids derivatives: potential modulators of multidrug resistance in cancer

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A series of new bisbenzylisoquinoline alkaloids was partially synthesized from tetrandrine and fangchinoline and evaluated for their ability to reverse P-glycoprotein-mediated multidrug resistance (MDR) in cancer cells. All the test compounds increased the intracellular accumulation rate of rhodamine 123 in MDR cells (Bel7402 and HCT8), and most exhibited more potent MDR-reversing activity relative to the reference compound verapamil. Compounds 8, 10, 13, and 14 enhanced intracellular accumulation of doxorubicin in Bel7402 and HCT8 cells.
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Keywords: P-glycoprotein; bisbenzylisoquinoline alkaloids; multidrug resistance

Document Type: Research Article

Affiliations: 1: Department of Chemistry of Medicinal Natural Products,West China College of Pharmacy, Sichuan University, Chengdu,610041, China 2: Department of Pharmacology,Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing,100050, China

Publication date: June 1, 2012

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