Investigating the anti-proliferative activity of styrylazanaphthalenes and azanaphthalenediones

Bioorg Med Chem. 2010 Apr 1;18(7):2664-71. doi: 10.1016/j.bmc.2010.02.025. Epub 2010 Feb 19.

Abstract

A group of styrylazanaphthalenes and azanaphthalenediones were synthesized and tested for their anti-proliferative activity. Most of the compounds were obtained with the use of microwave-assisted synthesis. The lipophilicity of the compounds was measured by RP-HPLC and their anti-proliferative activity was assayed against the human SK-N-MC neuroepithelioma and HCT116 human colon carcinoma cell lines. Active compounds were also tested in clonogenity and comet assays. Several quinazolinone and styrylquinazoline analogues were found to have markedly greater anti-proliferative activity than desferoxamine and cis-platin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Chromatography, High Pressure Liquid
  • Coloring Agents
  • Drug Screening Assays, Antitumor
  • Humans
  • Lipids / chemistry
  • Naphthalenes / chemical synthesis*
  • Naphthalenes / pharmacology*
  • Naphthoquinones / chemical synthesis*
  • Naphthoquinones / pharmacology*
  • Solubility
  • Styrenes / chemical synthesis*
  • Styrenes / pharmacology*
  • Tetrazolium Salts
  • Thiazoles
  • Tumor Stem Cell Assay

Substances

  • Antineoplastic Agents
  • Coloring Agents
  • Lipids
  • Naphthalenes
  • Naphthoquinones
  • Styrenes
  • Tetrazolium Salts
  • Thiazoles
  • thiazolyl blue