Design, synthesis, single-crystal and preliminary antitumor activity of novel arenesulfonylimidazolidin-2-ones

Bioorg Med Chem Lett. 2012 Mar 1;22(5):2008-14. doi: 10.1016/j.bmcl.2012.01.036. Epub 2012 Jan 21.

Abstract

Novel series of 1-(arenesulfonyl)imidazolidin-2-one (3a-i) and 1,3-bis(arenesulfonyl)imidazolidin-2-one (5a-i) have been synthesized and tested for their antitumor activity against 60 tumor cell lines taken from nine different organs. A significant inhibition for cancer cells was observed with series 5a-i compounds compared with the series 3a-i which showed a weak inhibition. Compounds 5a-i showed good inhibitory effect at the lung cancer HOP-92 and renal cancer CAKI-1 and UO-31 cell lines. Compound 5e showed remarkable broad-spectrum antitumor activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Crystallography, X-Ray
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Humans
  • Imidazolidines / chemical synthesis
  • Imidazolidines / chemistry*
  • Imidazolidines / pharmacology*
  • Models, Molecular
  • Neoplasms / drug therapy
  • Structure-Activity Relationship
  • Sulfonylurea Compounds / chemical synthesis
  • Sulfonylurea Compounds / chemistry
  • Sulfonylurea Compounds / pharmacology

Substances

  • Antineoplastic Agents
  • Imidazolidines
  • Sulfonylurea Compounds
  • ethylene urea