DNA-binding and DNA-cleaving properties of a synthetic model AGAGLU related to the antitumour drugs AMSA and bleomycin

Biochem Biophys Res Commun. 1988 Apr 29;152(2):695-702. doi: 10.1016/s0006-291x(88)80094-9.

Abstract

We have previously described two synthetic models gathering a simplified model of the complexing part of Bleomycin (Blm) and the intercalating moiety of m-AMSA. These molecules, namely AGGA and AGAMGA, do not seem able to cleave DNA as Blm does. The present work is devoted to the study of a new derivative, AGAGLU, which includes in its structure a judiciously chosen connector between the two parts of the molecule. This compound, the chelating and DNA-binding properties of which are described here, has been shown to induce single-strand breakage of duplex DNA in a high level.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoacridines / chemical synthesis
  • Aminoacridines / pharmacology*
  • Amsacrine / pharmacology*
  • Animals
  • Bleomycin / pharmacology*
  • Cattle
  • Chelating Agents / pharmacology
  • Circular Dichroism
  • Copper
  • DNA Damage*
  • DNA-Binding Proteins / pharmacology*
  • Drug Interactions
  • Electron Spin Resonance Spectroscopy
  • Free Radicals
  • Glucosamine / analogs & derivatives*
  • Glucosamine / chemical synthesis
  • Glucosamine / pharmacology
  • Spectrometry, Fluorescence
  • Thymus Gland

Substances

  • Aminoacridines
  • Chelating Agents
  • DNA-Binding Proteins
  • Free Radicals
  • Amsacrine
  • Bleomycin
  • (((amino-2-ethyl)-2-aminomethyl)-2-pyridine-6-carboxylhistidyl-gamma-(2-amino-2-deoxyglucosyl)glutamylglycylamino)-4-phenyl-1-aminoacridine
  • Copper
  • Glucosamine