Oxidative DNA base damage by the antitumor agent 3-amino-1,2,4-benzotriazine 1,4-dioxide (tirapazamine)

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2325-9. doi: 10.1016/s0960-894x(02)00468-7.

Abstract

Tirapazamine is a bioreductively activated DNA-damaging agent that selectively kills the hypoxic cells found in solid tumors. In this work, base excision repair enzymes were used to provide evidence that tirapazamine causes significant amounts of damage to both purine and pyrimidine residues in double-stranded DNA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • DNA / metabolism
  • DNA Damage / drug effects*
  • DNA Ligases / metabolism
  • Oxidation-Reduction
  • Purines / analysis
  • Pyrimidines / analysis
  • Restriction Mapping
  • Substrate Specificity
  • Tirapazamine
  • Triazines / pharmacology*

Substances

  • Antineoplastic Agents
  • Purines
  • Pyrimidines
  • Triazines
  • Tirapazamine
  • DNA
  • DNA Ligases