Functionalized chalcones as selective inhibitors of P-glycoprotein and breast cancer resistance protein.

@article{Liu2008FunctionalizedCA,
  title={Functionalized chalcones as selective inhibitors of P-glycoprotein and breast cancer resistance protein.},
  author={X L Liu and Hui-Wearn Tee and Mei-Lin Go},
  journal={Bioorganic & medicinal chemistry},
  year={2008},
  volume={16 1},
  pages={171-80}
}
A library of chalcones with basic functionalities were screened for inhibition of P-glycoprotein (Pgp, ABCB1) by the calcein-AM accumulation assay on MDCKII/MDR1 cells. Three members that had ring A substituted with 5-(1-ethylpiperidin-4-yl) and 2,4-dimethoxy groups were found to increase calcein-AM accumulation to a greater extent than verapamil, a Pgp inhibitor. These compounds were subsequently shown to enhance the uptake of doxorubicin by MCF-7 cells that over-expressed Pgp. However, when… CONTINUE READING