Synthesis of novel 5-substituted indirubins as protein kinases inhibitors

Bioorg Med Chem. 2006 Sep 15;14(18):6434-43. doi: 10.1016/j.bmc.2006.05.036. Epub 2006 Jun 8.

Abstract

In an effort to identify new pharmacological inhibitors of disease-relevant protein kinases with increased potency and selectivity, we synthesized and evaluated new 5-substituted indirubins. The effects of 34 indirubin derivatives on CDK1/cyclin B, CDK5/p25, and GSK-3, as well as on SH-SY5Y human neuroblastoma cell survival, were investigated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CDC2-CDC28 Kinases / antagonists & inhibitors*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Glycogen Synthase Kinase 3 / antagonists & inhibitors*
  • Humans
  • Indoles / chemical synthesis
  • Indoles / chemistry
  • Indoles / pharmacology
  • Molecular Structure
  • Molecular Weight
  • Protein Kinase Inhibitors / chemical synthesis*
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Starfish
  • Stereoisomerism
  • Structure-Activity Relationship
  • Swine

Substances

  • Indoles
  • Protein Kinase Inhibitors
  • CDC2-CDC28 Kinases
  • Glycogen Synthase Kinase 3
  • indirubin