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Keywords:

  • ABC transporters;
  • breast cancer resistance proteins;
  • inhibitors;
  • sonogashira couplings;
  • syntheses
Thumbnail image of graphical abstract

ABC, it′s easy as 1 2 3! Bioisosteric replacement of the anilide core by an indole moiety considerably increased stability and gave potent and selective ABCG2 (BCRP) inhibitors. Some compounds are superior to the reference substances fumitremorgin C and Ko143 in terms of potency and efficacy and are the most potent ABCG2 modulators reported so far.