title: Synthesis of a resorcylic acid lactone (RAL) library using fluorous-mixture synthesis and profile of its selectivity against a panel of kinases.
abstract: A library of resorcylic acid lactones (RAL) containing a cis-enone moiety targeting kinases bearing a cysteine residue within the ATP-binding pocket was prepared using a fluorous-mixture synthesis and evaluated against a panel of 19 kinases thus providing important structure-activity trends. Two new analogues were then profiled for their selectivity against a panel of 402 kinases providing the broadest evaluation of this pharmacophores' selectivity.
authors.affiliation: Institut de Science et Ingénierie Supramoléculaires (ISIS-UMR 7006), Université de Strasbourg-CNRS, 8 allée Gaspard Monge, 67000 Strasbourg, France.
authors.forename: Rajamalleswaramma
authors.initials: R
authors.lastname: Jogireddy
authors.forename: Pierre-Yves
authors.initials: PY
authors.lastname: Dakas
authors.forename: Gaëlle
authors.initials: G
authors.lastname: Valot
authors.forename: Sofia
authors.initials: S
authors.lastname: Barluenga
authors.forename: Nicolas
authors.initials: N
authors.lastname: Winssinger
mesh_terms: D000255:Adenosine Triphosphate / Q000737:chemistry; D005461:Fluorine / Q000737:chemistry*; D062385:Hydroxybenzoates / Q000737:chemistry*; D007783:Lactones / Q000138:chemical synthesis* / Q000737:chemistry; D010770:Phosphotransferases / Q000378:metabolism*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D054852:Small Molecule Libraries; D013329:Structure-Activity Relationship
chemical_list: D062385:Hydroxybenzoates; D007783:Lactones; D047428:Protein Kinase Inhibitors; D054852:Small Molecule Libraries; D005461:Fluorine; D000255:Adenosine Triphosphate; D010770:Phosphotransferases