title: Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004.
abstract: New heteroarylcarboxamide head groups substituted with two aromatic rings analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Potent inhibitors of RON tyrosine kinase with various level of selectivity for c-Met RTK were obtained.
authors.affiliation: Laboratoires ChemRF Inc./ChemRF Laboratories Inc., 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada.
authors.forename: Franck
authors.initials: F
authors.lastname: Raeppel
authors.affiliation: Laboratoires ChemRF Inc./ChemRF Laboratories Inc., 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: Laboratoires ChemRF Inc./ChemRF Laboratories Inc., 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada.
authors.forename: Eric
authors.initials: E
authors.lastname: Therrien
mesh_terms: D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006574:Heterocyclic Compounds, 2-Ring / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D006574:Heterocyclic Compounds, 2-Ring; C000605132:LCRF-0004; D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; C080835:RON protein; D020794:Receptor Protein-Tyrosine Kinases
keywords: Head group; Molecular docking; Oncology; RON; RON homology model; RTK inhibitors; c-Met