Synthesis of novel bis-anthraquinone derivatives and their biological evaluation as antitumor agents

Arch Pharm Res. 2013 May;36(5):573-8. doi: 10.1007/s12272-013-0074-x. Epub 2013 Mar 8.

Abstract

Cancer has become a major worldwide problem and drug resistance now is one of the most important problems in treatment of cancer. Anthraquinone derivatives represent one of the most important drugs that can be used in treatment of many types of cancer. In this study two series of novel bis-anthraquinone derivatives have been synthesized. Five of these compounds were chosen to be evaluated for their antitumor activity against human cancer cell lines by the National Cancer Institute (NCI, USA). Marked activity was shown for the tested compounds(2-6). The most active one was compound 6 with mean value -67.00 against all cell lines. Compounds 7 and 8 were found inactive.

MeSH terms

  • Anthraquinones / chemical synthesis*
  • Anthraquinones / chemistry
  • Anthraquinones / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Anthraquinones
  • Antineoplastic Agents