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Keywords:

  • antitumor agents;
  • glycosylation;
  • photoreaction;
  • polyketides;
  • streptomyces chartreusis
Thumbnail image of graphical abstract

Light on DNA intercalators: Molecular modeling and mutasynthesis were employed to rationally tailor the antitumoral agent chartreusin into a vinyl-substituted derivative. Exposure with visible light dramatically improved antiproliferative activities owing to covalent binding with DNA and induction of apoptosis. The results hold promise for a more efficient chemotherapy, in particular for selectively treating tumors with light probes.