Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles

Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7. doi: 10.1016/j.bmcl.2003.12.002.

Abstract

The discovery, synthesis, potential binding mode, and in vitro kinase profile of 3-(3-bromo-4-hydroxy-5-(2'-methoxyphenyl)-benzylidene)-5-bromo-1,3-dihydro-pyrrolo[2,3-b]pyridin-2-one, 3-[(1-methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-b]-pyridin-2-one as potent TrkA inhibitors are discussed.

MeSH terms

  • CDC2-CDC28 Kinases / antagonists & inhibitors
  • Cyclin-Dependent Kinase 2
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Indoles / chemical synthesis
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Models, Molecular
  • Molecular Structure
  • Proto-Oncogene Proteins c-raf / antagonists & inhibitors
  • Receptor, trkA / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Substrate Specificity

Substances

  • Enzyme Inhibitors
  • Indoles
  • Receptor, trkA
  • Proto-Oncogene Proteins c-raf
  • CDC2-CDC28 Kinases
  • Cyclin-Dependent Kinase 2