Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/26110
Title: Synthesis of methylated quercetin derivatives and their reversal activities on P-gp- and BCRP-mediated multidrug resistance tumour cells
Authors: Yuan, J
Wong, ILK
Jiang, T
Wang, SW
Liu, T
Wen, BJ
Chow, LMC 
Sheng, BW
Keywords: BCRP
Methylated quercetin derivatives
MRP1
Multidrug resistance (MDR)
P-gp
Quercetin
Issue Date: 2012
Publisher: Elsevier Masson
Source: European journal of medicinal chemistry, 2012, v. 54, p. 413-422 How to cite?
Journal: European journal of medicinal chemistry 
Abstract: 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.
URI: http://hdl.handle.net/10397/26110
ISSN: 0223-5234
EISSN: 1768-3254
DOI: 10.1016/j.ejmech.2012.05.026
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