title: The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors.
abstract: Substituted 4-(3-hydroxyanilino)-quinoline compounds, initially identified as small-molecule inhibitors of src family kinases, have been evaluated as potential inhibitors of RET kinase. Three compounds, 38, 31, and 40, had K(i)'s of 3, 25, and 50 nM in an in vitro kinase assay; while a cell based kinase assay showed K(i)'s of 300, 100, and 45 nM, respectively. These compounds represent potential new leads for the treatment of medullary and papillary thyroid cancer.
authors: GlaxoSmithKline, Molecular Discovery Research Chemistry, 5 Moore Drive, Research Triangle Park, NC 27709, USA.
authors: R
authors: R
authors: Graham Robinett
authors: Alex J
authors: AJ
authors: Freemerman
authors: Michael A
authors: MA
authors: Skinner
authors: Lisa
authors: L
authors: Shewchuk
authors: Karen
authors: K
authors: Lackey
mesh_terms: D001665:Binding Sites; D006801:Humans; D008958:Models, Molecular; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D051096:Proto-Oncogene Proteins c-ret / Q000037:antagonists & inhibitors* / Q000737:chemistry; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D047428:Protein Kinase Inhibitors; D011804:Quinolines; D051096:Proto-Oncogene Proteins c-ret; C099282:RET protein, human