Design and synthesis of close analogs of LCRF-0004, a potent and selective RON receptor tyrosine kinase inhibitor

  • Bioorg Med Chem Lett. 2015 Jun 15;25(12):2527-31. doi: 10.1016/j.bmcl.2015.04.056.
Stéphane L Raeppel  1 Franck Raeppel  2 Eric Therrien  2
Affiliations
  • 1. ChemRF Laboratories, 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada. Electronic address: [email protected].
  • 2. ChemRF Laboratories, 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada.
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.

Keywords
Head group; Oncology; RON; RTK inhibitors; Thieno[3,2-b]pyridine scaffold; c-Met.
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