Discovery of thiophene inhibitors of polo-like kinase

Bioorg Med Chem Lett. 2009 Feb 1;19(3):1018-21. doi: 10.1016/j.bmcl.2008.11.041. Epub 2008 Nov 18.

Abstract

The discovery and development of a series of thiophenes as potent and selective inhibitors of PLK is described. Identification and characterization of 2, a useful in vitro PLK inhibitor tool compound, is also presented.

MeSH terms

  • Animals
  • Cell Cycle
  • Cell Cycle Proteins / antagonists & inhibitors*
  • Cell Cycle Proteins / chemistry
  • Cell Line, Tumor
  • Cell Proliferation
  • Chemistry, Pharmaceutical / methods*
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Mice
  • Mitosis
  • Models, Chemical
  • Molecular Conformation
  • Polo-Like Kinase 1
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Protein Serine-Threonine Kinases / chemistry
  • Proto-Oncogene Proteins / antagonists & inhibitors*
  • Proto-Oncogene Proteins / chemistry
  • Thiophenes / antagonists & inhibitors*
  • Thiophenes / chemistry

Substances

  • Cell Cycle Proteins
  • Enzyme Inhibitors
  • Proto-Oncogene Proteins
  • Thiophenes
  • Protein Serine-Threonine Kinases