Synthesis, characterization and anti-tumor activity of moxifloxacin-copper complexes against breast cancer cell lines

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1802-6. doi: 10.1016/j.bmcl.2011.01.061. Epub 2011 Jan 21.

Abstract

Novel moxifloxacin-copper complexes were synthesized, characterized and screened for anti-proliferative and apoptosis-inducing activity against multiple human breast cancer cell lines (hormone-dependent MCF-7 and T47D as well as hormone-independent MDA-MB-231 and BT-20). The results indicated that the parent compound moxifloxacin (1) does not exert any inhibitory activity against breast cancer cell lines examined. On the other hand, the copper conjugate 2 and its nitrogen adducts 3-5 exerted growth inhibitory and apoptosis-inducing activity against breast cancer cell lines without any substantial effect on non-tumorigenic breast epithelial cells MCF-10A at equimolar concentration, suggesting a cancer cell-specific activity. BT-20 cells were more sensitive to compounds 2 and 3, while compounds 4 and 5 exerted significant anti-proliferative and apoptosis-inducing effects on T47D, MDA-MB-231 and BT-20 cell lines. Our results suggest that these novel compounds could be useful for the treatment of breast cancer in the future.

MeSH terms

  • Apoptosis / drug effects
  • Aza Compounds / chemical synthesis*
  • Aza Compounds / chemistry
  • Aza Compounds / pharmacology*
  • Breast Neoplasms / pathology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Copper / chemistry*
  • Drug Screening Assays, Antitumor
  • Female
  • Fluoroquinolones
  • Humans
  • Moxifloxacin
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Spectrophotometry, Infrared

Substances

  • Aza Compounds
  • Fluoroquinolones
  • Quinolines
  • Copper
  • Moxifloxacin