On the mechanism of reductive activation in the mode of action of some anticancer drugs

Biochimie. 1982 Jul;64(7):457-75. doi: 10.1016/s0300-9084(82)80162-4.


Bioactivation of a number of DNA-specific antitumor drugs depends on oxidoreduction. Bleomycin, neocarzinostatin and anthracycline glycosides are the best known among such drugs in terms of reductive activation processes. Their reduction results in short-lived radical or electrophilic intermediates attacking DNA stereospecifically. The physico-chemical properties of these drugs and the nature of DNA damage are reviewed. Models for DNA-intercalation, electron-donor systems involved in drug metabolisation, and the role of oxygen in radical reactions, are discussed in the light of recent reports.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antibiotics, Antineoplastic / metabolism*
  • Antineoplastic Agents / metabolism*
  • Biotransformation
  • Bleomycin / metabolism*
  • Chemical Phenomena
  • Chemistry
  • DNA / metabolism
  • Free Radicals
  • Naphthacenes / metabolism
  • Oxidation-Reduction
  • Oxygen / metabolism
  • Zinostatin / metabolism*


  • Antibiotics, Antineoplastic
  • Antineoplastic Agents
  • Free Radicals
  • Naphthacenes
  • Bleomycin
  • DNA
  • Zinostatin
  • Oxygen