Inhibition of eEF2-K by thieno[2,3-b]pyridine analogues

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2283-6. doi: 10.1016/j.bmcl.2010.02.005. Epub 2010 Feb 6.

Abstract

Several series of thieno[2-3-b]pyridine analogues were synthesized and screened for inhibitory activity against eukaryotic elongation factor-2 kinase (eEF2-K). Modifications around several regions of the lead molecules were made, with a ring fusion adjacent to the nitrogen on the thienopyridine core being critical for activity. The most active compound 34 shows an IC(50) of 170 nM against eEF2-K in vitro.

MeSH terms

  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Elongation Factor 2 Kinase / antagonists & inhibitors*
  • Elongation Factor 2 Kinase / metabolism*
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Pyridines / chemistry*
  • Pyridines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Pyridines
  • thienopyridine
  • Elongation Factor 2 Kinase