title: Discovery of a novel series of quinoxalines as inhibitors of c-Met kinase.
abstract: A series of quinoxaline inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and optimisation of the series was performed on the basis of this structure. Future directions for development of the series are discussed together with the identification of a novel quinoline scaffold.
authors.affiliation: UCB Celltech, 216 Bath Road, Slough SL1 3WE, United Kingdom. john.porter@ucb-group.com
authors.forename: John
authors.initials: J
authors.lastname: Porter
authors.forename: Simon
authors.initials: S
authors.lastname: Lumb
authors.forename: Fabien
authors.initials: F
authors.lastname: Lecomte
authors.forename: James
authors.initials: J
authors.lastname: Reuberson
authors.forename: Anne
authors.initials: A
authors.lastname: Foley
authors.forename: Mark
authors.initials: M
authors.lastname: Calmiano
authors.forename: Kelly
authors.initials: K
authors.lastname: le Riche
authors.forename: Helen
authors.initials: H
authors.lastname: Edwards
authors.forename: Jean
authors.initials: J
authors.lastname: Delgado
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Franklin
authors.forename: Jose M
authors.initials: JM
authors.lastname: Gascon-Simorte
authors.forename: Alison
authors.initials: A
authors.lastname: Maloney
authors.forename: Christoph
authors.initials: C
authors.lastname: Meier
authors.forename: Mark
authors.initials: M
authors.lastname: Batchelor
mesh_terms: D018360:Crystallography, X-Ray; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D019859:Proto-Oncogene Proteins c-met / Q000037:antagonists & inhibitors*; D011810:Quinoxalines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011810:Quinoxalines; D019859:Proto-Oncogene Proteins c-met