4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors

Bioorg Med Chem Lett. 2009 May 1;19(9):2504-8. doi: 10.1016/j.bmcl.2009.03.034. Epub 2009 Mar 14.

Abstract

The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity.

MeSH terms

  • Adenosine Triphosphate / chemistry
  • Binding Sites
  • Chemistry, Pharmaceutical / methods*
  • Drug Design
  • Humans
  • I-kappa B Kinase / antagonists & inhibitors*
  • Indoles / chemical synthesis*
  • Indoles / pharmacology*
  • Inhibitory Concentration 50
  • Models, Chemical
  • Models, Molecular
  • Molecular Structure
  • Protein Binding
  • Structure-Activity Relationship
  • Sulfonamides / chemistry

Substances

  • 7-azaindole dimer
  • Indoles
  • Sulfonamides
  • Adenosine Triphosphate
  • I-kappa B Kinase