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Keywords:

  • artemisinin;
  • binding studies;
  • cytotoxicity;
  • DNA;
  • molecular modelling
Thumbnail image of graphical abstract

Greater than the sum of its parts: Artemisinins are currently in phase I–II clinical trials against breast, colorectal and non-small-cell lung cancers. In an attempt to offer increased specificity, a series of hybrid artemisinin–polypyrrole minor groove binder conjugates are described. DNA binding/modelling studies and preliminary biological evaluation give insights into their mechanism of action and the potential of this strategy.