Scaffold oriented synthesis. Part 4: Design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing …

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. 1480 - 1483

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Citation Number: 18

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.