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

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

  • Bioorg Med Chem Lett. 2009 Feb 1;19(3):1004-8. doi: 10.1016/j.bmcl.2008.11.058.
Kyle A Emmitte 1,  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 Jr,  Ganesh S Moorthy,  Scott H Dickerson,  Anne M Hassell,  M Anthony Leesnitzer,  Lisa M Shewchuk,  Arthur Groy,  Jason L Rowand,  Kelly Anderson,  Charity L Atkins,  Jingsong Yang,  Peter Sabbatini,  Rakesh Kumar
Affiliations

Affiliation

  • 1 GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA. kyle.a.emmitte@Vanderbilt.edu
PMID: 19101143 DOI: 10.1016/j.bmcl.2008.11.058
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.

Figures