title: Design and synthesis of close analogs of LCRF-0004, a potent and selective RON receptor tyrosine kinase inhibitor.
abstract: New carboxamide head group analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Potent and selective inhibitors of RON enzyme versus c-Met RTK were obtained.
authors.affiliation: ChemRF Laboratories, 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada. Electronic address: stephane.raeppel@gmail.com.
authors.forename: Stéphane L
authors.initials: SL
authors.lastname: Raeppel
authors.affiliation: ChemRF Laboratories, 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada.
authors.forename: Franck
authors.initials: F
authors.lastname: Raeppel
authors.affiliation: ChemRF Laboratories, 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada.
authors.forename: Eric
authors.initials: E
authors.lastname: Therrien
mesh_terms: D000577:Amides / Q000737:chemistry; D001665:Binding Sites; D015195:Drug Design; D006574:Heterocyclic Compounds, 2-Ring / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D062105:Molecular Docking Simulation; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D017434:Protein Structure, Tertiary; D019859:Proto-Oncogene Proteins c-met / Q000037:antagonists & inhibitors / Q000378:metabolism; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000577:Amides; D006574:Heterocyclic Compounds, 2-Ring; C000605132:LCRF-0004; D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D019859:Proto-Oncogene Proteins c-met; C080835:RON protein; D020794:Receptor Protein-Tyrosine Kinases
keywords: Head group; Oncology; RON; RTK inhibitors; Thieno[3,2-b]pyridine scaffold; c-Met