2. Academic Validation
  3. Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004

Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004

  • Bioorg Med Chem Lett. 2015 Sep 15;25(18):3810-5. doi: 10.1016/j.bmcl.2015.07.080.
Franck Raeppel 1,  Stéphane L Raeppel 2,  Eric Therrien 1
Affiliations

Affiliations

  • 1 Laboratoires ChemRF Inc./ChemRF Laboratories Inc., 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada.
  • 2 Laboratoires ChemRF Inc./ChemRF Laboratories Inc., 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada. Electronic address: [email protected].
PMID: 26243370 DOI: 10.1016/j.bmcl.2015.07.080
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.

Keywords

Head group; Molecular docking; Oncology; RON; RON homology model; RTK inhibitors; c-Met.

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