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Keywords:

  • antitumor agents;
  • duocarmycins;
  • hypoxia;
  • phosphates;
  • prodrugs
Thumbnail image of graphical abstract

Hitting the hypoxic target: Combining a nitro prodrug with a water-soluble phosphate converts duocarmycin analogues from highly toxic DNA-alkylating agents to highly selective antitumor compounds. These prodrugs (see scheme) have outstanding activity against hypoxic tumor cells in vivo, cells which are usually considered the most resistant to conventional therapy.