Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions

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

doi:10.1016/j.bmcl.2011.01.007

Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1476-9. doi: 10.1016/j.bmcl.2011.01.007. 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. irini.zanze@abbott.com

PMID: 21282054
DOI: 10.1016/j.bmcl.2011.01.007

Abstract

We report the synthesis and biological evaluation of 5-substituted indazoles and amino indazoles as kinase inhibitors. The compounds were synthesized in a parallel synthesis fashion from readily available starting materials employing [2+3] cycloaddition reactions and were evaluated against a panel of kinase assays. Potent inhibitors were identified for numerous kinases such as Rock2, Gsk3β, Aurora2 and Jak2.

MeSH terms

Cyclization
Drug Design*
Indazoles* / chemical synthesis
Indazoles* / pharmacology
Molecular Structure
Protein Kinase Inhibitors* / chemical synthesis
Protein Kinase Inhibitors* / pharmacology

Substances

Indazoles
Protein Kinase Inhibitors