Synthesis and characterization of a novel iNOS/Akt inhibitor Se,Se'-1,4-phenylenebis(1,2-ethanediyl)bisisoselenourea (PBISe)--against colon cancer

Bioorg Med Chem Lett. 2010 Mar 15;20(6):2038-43. doi: 10.1016/j.bmcl.2009.09.071. Epub 2009 Sep 22.

Abstract

Our studies demonstrate that substitution of sulfur with selenium in known iNOS inhibitor increases the compound's potency by several folds in variety of different cancers cell lines tested. Hence, this approach may be used as a strategy to increase the efficacy of the anticancer agents.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Colonic Neoplasms / enzymology
  • Colonic Neoplasms / pathology
  • Colonic Neoplasms / prevention & control*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Nitric Oxide Synthase Type II / antagonists & inhibitors*
  • Organoselenium Compounds / chemical synthesis*
  • Organoselenium Compounds / chemistry
  • Organoselenium Compounds / pharmacology
  • Organoselenium Compounds / therapeutic use*
  • Proto-Oncogene Proteins c-akt / antagonists & inhibitors*
  • Urea / analogs & derivatives*
  • Urea / chemical synthesis
  • Urea / chemistry
  • Urea / pharmacology
  • Urea / therapeutic use

Substances

  • Enzyme Inhibitors
  • Organoselenium Compounds
  • S,S'-1,4-phenylenebis(1,2-ethanediyl)bisisoselenourea
  • Urea
  • Nitric Oxide Synthase Type II
  • Proto-Oncogene Proteins c-akt