DNA binding specificity and cytotoxicity of novel antitumor agent Ge132 derivatives

Bioorg Med Chem Lett. 2005 Jun 15;15(12):2962-5. doi: 10.1016/j.bmcl.2005.04.053.

Abstract

A series of Ge132 derivatives have shown enhanced antitumor activity. Previous studies suggest that DNA can be their primary target. Here we show direct evidence that two newly synthesized Ge132 derivatives can intercalate into DNA. Unexpected methyl substitution effect of the novel derivatives on DNA sequence selectivity and cytotoxicity was observed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / metabolism*
  • Cattle
  • Cell Cycle / drug effects
  • Cell Proliferation / drug effects
  • DNA / chemistry
  • DNA / metabolism*
  • Drug Screening Assays, Antitumor
  • Germanium
  • Humans
  • Inhibitory Concentration 50
  • Intercalating Agents / metabolism*
  • Male
  • Organometallic Compounds / metabolism*
  • Propionates
  • Prostatic Neoplasms / metabolism*
  • Prostatic Neoplasms / pathology
  • Quinolines / chemistry
  • Quinolines / metabolism
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Intercalating Agents
  • Organometallic Compounds
  • Propionates
  • Quinolines
  • Germanium
  • propagermanium
  • DNA