title: 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.
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.
authors.affiliation: Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60044, USA. irini.zanze@abbott.com
authors.forename: Irini
authors.initials: I
authors.lastname: Akritopoulou-Zanze
authors.forename: Brian D
authors.initials: BD
authors.lastname: Wakefield
authors.forename: Alan
authors.initials: A
authors.lastname: Gasiecki
authors.forename: Douglas
authors.initials: D
authors.lastname: Kalvin
authors.forename: Eric F
authors.initials: EF
authors.lastname: Johnson
authors.forename: Peter
authors.initials: P
authors.lastname: Kovar
authors.forename: Stevan W
authors.initials: SW
authors.lastname: Djuric
mesh_terms: D015195:Drug Design; D006571:Heterocyclic Compounds / Q000737:chemistry*; D007191:Indazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D006571:Heterocyclic Compounds; D007191:Indazoles; D047428:Protein Kinase Inhibitors