Synthesis and biological evaluation of rhodanine derivatives as PRL-3 inhibitors

Bioorg Med Chem Lett. 2006 Jun 1;16(11):2996-9. doi: 10.1016/j.bmcl.2006.02.060. Epub 2006 Mar 10.

Abstract

A series of rhodanine derivatives was synthesized and evaluated for their ability to inhibit PRL-3. Benzylidene rhodanine derivative showed good biological activity, while compound 5e was the most active in this series exhibiting an IC50 value of 0.9 microM in vitro and showed a reduced invasion in cell-based assay.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemistry
  • Animals
  • Cell Line, Tumor
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Mice
  • Molecular Structure
  • Naphthalenes / chemistry
  • Protein Binding
  • Protein Tyrosine Phosphatases / antagonists & inhibitors*
  • Protein Tyrosine Phosphatases / classification
  • Protein Tyrosine Phosphatases / metabolism*
  • Rhodanine / chemical synthesis
  • Rhodanine / chemistry*
  • Rhodanine / pharmacology*
  • Structure-Activity Relationship

Substances

  • Aldehydes
  • Enzyme Inhibitors
  • Naphthalenes
  • salicylaldehyde
  • naphthalene
  • Rhodanine
  • Protein Tyrosine Phosphatases