title: Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.
abstract: The discovery, synthesis, potential binding mode, and in vitro kinase profile of 3-(3-bromo-4-hydroxy-5-(2'-methoxyphenyl)-benzylidene)-5-bromo-1,3-dihydro-pyrrolo[2,3-b]pyridin-2-one, 3-[(1-methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-b]-pyridin-2-one as potent TrkA inhibitors are discussed.
authors.affiliation: GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA.
authors.forename: Edgar R
authors.initials: ER
authors.lastname: Wood
authors.forename: Lee
authors.initials: L
authors.lastname: Kuyper
authors.forename: Kimberly G
authors.initials: KG
authors.lastname: Petrov
authors.forename: Robert N
authors.initials: RN
authors.lastname: Hunter
authors.forename: Philip A
authors.initials: PA
authors.lastname: Harris
authors.forename: Karen
authors.initials: K
authors.lastname: Lackey
mesh_terms: D042846:CDC2-CDC28 Kinases / Q000037:antagonists & inhibitors; D051357:Cyclin-Dependent Kinase 2; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D019908:Proto-Oncogene Proteins c-raf / Q000037:antagonists & inhibitors; D020917:Receptor, trkA / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; D020917:Receptor, trkA; D019908:Proto-Oncogene Proteins c-raf; D042846:CDC2-CDC28 Kinases; D051357:Cyclin-Dependent Kinase 2