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

I Akritopoulou-Zanze, BD Wakefield, A Gasiecki…

Index: Akritopoulou-Zanze, Irini; Wakefield, Brian D.; Gasiecki, Alan; Kalvin, Douglas; Johnson, Eric F.; Kovar, Peter; Djuric, Stevan W. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 5 p. 1476 - 1479

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Citation Number: 11

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.