Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)

Kyle A. Emmitte, Brian J. Wilson, Erich W. Baum, Holly K. Emerson, Kevin W. Kuntz, Kristen E. Nailor, James M. Salovich, Stephon C. Smith, Mui Cheung, Roseanne M. Gerding, Kirk L. Stevens, David E. Uehling, Robert A. Mook, Ganesh S. Moorthy, Scott H. Dickerson, Anne M. Hassell, M. Anthony Leesnitzer, Lisa M. Shewchuk, Arthur Groy, Jason L. RowandKelly Anderson, Charity L. Atkins, Jingsong Yang, Peter Sabbatini, Rakesh Kumar

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Abstract

The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimized compound is also highlighted.

Original languageEnglish
Pages (from-to)1004-1008
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number3
DOIs
StatePublished - 1 Feb 2009

Keywords

  • Cancer
  • Imidazo[1,2-a]pyridine
  • Insulin receptor
  • Insulin-like growth factor-1 receptor
  • Kinase inhibitor

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    Emmitte, K. A., Wilson, B. J., Baum, E. W., Emerson, H. K., Kuntz, K. W., Nailor, K. E., Salovich, J. M., Smith, S. C., Cheung, M., Gerding, R. M., Stevens, K. L., Uehling, D. E., Mook, R. A., Moorthy, G. S., Dickerson, S. H., Hassell, A. M., Anthony Leesnitzer, M., Shewchuk, L. M., Groy, A., ... Kumar, R. (2009). Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). Bioorganic and Medicinal Chemistry Letters, 19(3), 1004-1008. https://doi.org/10.1016/j.bmcl.2008.11.058