Synthesis of novel 5-substituted indirubins as protein kinases inhibitors

Anne Beauchard; Yoan Ferandin; Stéphane Frère; Olivier Lozach; Mélina Blairvacq; Laurent Meijer; Valérie Thiéry; Thierry Besson

doi:10.1016/j.bmc.2006.05.036

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.

Authors

Anne Beauchard¹, Yoan Ferandin, Stéphane Frère, Olivier Lozach, Mélina Blairvacq, Laurent Meijer, Valérie Thiéry, Thierry Besson

Affiliation

¹ Laboratoire de Biotechnologies et de Chimie Bio-organique, FRE CNRS 2766, UFR Sciences Fondamentales et Sciences pour l'Ingénieur, Université de La Rochelle, Bâtiment Marie Curie, 17042 La Rochelle, France.

PMID: 16759872
DOI: 10.1016/j.bmc.2006.05.036

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