The combination of quinazoline and chalcone moieties leads to novel potent heterodimeric modulators of breast cancer resistance protein (BCRP/ABCG2).

@article{Kraege2016TheCO,
  title={The combination of quinazoline and chalcone moieties leads to novel potent heterodimeric modulators of breast cancer resistance protein (BCRP/ABCG2).},
  author={Stefanie Kraege and Katja Stefan and Kapil Juvale and Thomas Ross and Thomas Willmes and Michael Wiese},
  journal={European journal of medicinal chemistry},
  year={2016},
  volume={117},
  pages={212-29}
}
During the last decade it has been found that chalcones and quinazolines are promising inhibitors of ABCG2. The combination of these two scaffolds offers a new class of heterocyclic compounds with potentially high inhibitory activity against ABCG2. For this purpose we investigated 22 different heterodimeric derivatives. In this series only methoxy groups were used as substituents as these had been proven superior for inhibitory activity of chalcones. All compounds were tested for their… CONTINUE READING
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