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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
Authors:Akritopoulou-Zanze Irini  Wakefield Brian D  Gasiecki Alan  Kalvin Douglas  Johnson Eric F  Kovar Peter  Djuric Stevan W
Affiliation:Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60044, USA
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.
Keywords:Kinase scaffolds   Kinase inhibitors   Rock2 inhibitors   Gsk3β inhibitors   Aurora2 inhibitors   Jak2 inhibitors   [2+3] Cycloadditions   Triazoles   Isoxazoles
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