Flavonoid-related modulators of multidrug resistance: synthesis, pharmacological activity, and structure-activity relationships.

@article{Fert1999FlavonoidrelatedMO,
  title={Flavonoid-related modulators of multidrug resistance: synthesis, pharmacological activity, and structure-activity relationships.},
  author={Jacques Fert{\'e} and J M K{\"u}hnel and Gervais Chapuis and Yves M Rolland and Guy Lewin and M A Schwaller},
  journal={Journal of medicinal chemistry},
  year={1999},
  volume={42 3},
  pages={478-89}
}
A series of 28 flavonoid derivatives containing a N-benzylpiperazine chain have been synthesized and tested for their ability to modulate multidrug resistance (MDR) in vitro. At 5 microM, most compounds potentiated doxorubicin cytotoxicity on resistant K562/DOX cells. They were also able to increase the intracellular accumulation of JC-1, a fluorescent molecule recently described as a probe of P-glycoprotein-mediated MDR. This suggests that these compounds act, at least in part, by inhibiting P… CONTINUE READING

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