Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue -, Pages 413-422Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.05.026
Keywords
Quercetin; Methylated quercetin derivatives; Multidrug resistance (MDR); P-gp; BCRP; MRP1
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Funding
- National Natural Science Foundation of China [NSFC 81172926]
- General Research Fund of the Research Grant Council of Hong Kong [B-Q16G]
- Special Fund for Marine Scientific Research in the Public Interest of China [201005024]
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Three methylated quercetins and a series of O-3 substituted 5,7,3',4'-tetra-O-methylated quercetin derivatives have been synthesized and evaluated on the modulating activity of P-gp, BCRP and MRP1 in cancer cell lines. Compound 17 (with a 2-((4-methoxybenzoyl)oxy)ethyl at O-3) is the most potent P-gp modulator. Three derivatives, compound 9 (3,7,3',4'-tetra-O-methylated quercetin), compound 14 (with a 2-((3-oxo-3-(3,4,5trimethoxyphenyl)prop-1-en-1-yl)oxy)ethyl at O-3) and compound 17, consistently exhibited promising BCRP-modulating activity. Interestingly, compound 17 was found to be equipotent against both P-gp and BCRP Importantly, these synthetic quercetin derivatives did not exhibit any inherent cytotoxicity to cancer cell lines or normal mouse fibroblast cell lines. These quercetin derivatives can be employed as safe and effective modulators of P-gp- or BCRP-mediated drug resistance in cancer. (C) 2012 Elsevier Masson SAS. All rights reserved.
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