Synthesis of methylated quercetin derivatives and their reversal activities on P-gp- and BCRP-mediated multidrug resistance tumour cells.

@article{Yuan2012SynthesisOM,
  title={Synthesis of methylated quercetin derivatives and their reversal activities on P-gp- and BCRP-mediated multidrug resistance tumour cells.},
  author={Jian Yuan and Iris L. K. Wong and Tao Jiang and Si Wang and Tao Liu and Bin Wen and Larry M. C. Chow and Biao Wan Sheng},
  journal={European journal of medicinal chemistry},
  year={2012},
  volume={54},
  pages={413-22}
}
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… CONTINUE READING
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