Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions

Irini Akritopoulou-Zanze; Brian D Wakefield; Alan Gasiecki; Douglas Kalvin; Eric F Johnson; Peter Kovar; Stevan W Djuric

doi:10.1016/j.bmcl.2011.01.001

Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1480-3. doi: 10.1016/j.bmcl.2011.01.001. Epub 2011 Jan 11.

Authors

Irini Akritopoulou-Zanze¹, Brian D Wakefield, Alan Gasiecki, Douglas Kalvin, Eric F Johnson, Peter Kovar, Stevan W Djuric

Affiliation

¹ Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60044, USA. [email protected]

PMID: 21288717
DOI: 10.1016/j.bmcl.2011.01.001

Abstract

We report the synthesis and biological evaluation of 5-substituted indazoles as kinase inhibitors. The compounds were synthesized in a parallel synthesis fashion from readily available starting materials employing heterocycle forming and multicomponent reactions and were evaluated against a panel of kinase assays. Potent inhibitors were identified for Gsk3β, Rock2, and Egfr.

MeSH terms

Drug Design*
Heterocyclic Compounds / chemistry*
Indazoles / chemical synthesis*
Indazoles / chemistry
Indazoles / pharmacology
Molecular Structure
Protein Kinase Inhibitors / chemical synthesis*
Protein Kinase Inhibitors / chemistry
Protein Kinase Inhibitors / pharmacology
Structure-Activity Relationship

Substances

Heterocyclic Compounds
Indazoles
Protein Kinase Inhibitors