title: The azaindole framework in the design of kinase inhibitors.
abstract: This review article illustrates the growing use of azaindole derivatives as kinase inhibitors and their contribution to drug discovery and innovation. The different protein kinases which have served as targets and the known molecules which have emerged from medicinal chemistry and Fragment-Based Drug Discovery (FBDD) programs are presented. The various synthetic routes used to access these compounds and the chemical pathways leading to their synthesis are also discussed. An analysis of their mode of binding based on X-ray crystallography data gives structural insights for the design of more potent and selective inhibitors.
authors.affiliation: Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS 7311, Orléans F-45067, France. jean-yves.merour@univ-orleans.fr.
authors.forename: Jean-Yves
authors.initials: JY
authors.lastname: Mérour
authors.affiliation: Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS 7311, Orléans F-45067, France. frederic.buron@univ-orleans.fr.
authors.forename: Frédéric
authors.initials: F
authors.lastname: Buron
authors.affiliation: Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS 7311, Orléans F-45067, France. karen.ple@univ-orleans.fr.
authors.forename: Karen
authors.initials: K
authors.lastname: Plé
authors.affiliation: Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS 7311, Orléans F-45067, France. pascal.bonnet@univ-orleans.fr.
authors.forename: Pascal
authors.initials: P
authors.lastname: Bonnet
authors.affiliation: Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS 7311, Orléans F-45067, France. sylvain.routier@univ-orleans.fr.
authors.forename: Sylvain
authors.initials: S
authors.lastname: Routier
mesh_terms: D000818:Animals; D001372:Aza Compounds / Q000737:chemistry*; D015195:Drug Design; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D047428:Protein Kinase Inhibitors / Q000737:chemistry*
chemical_list: D001372:Aza Compounds; D007211:Indoles; D047428:Protein Kinase Inhibitors; C030374:indole