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

…, JM Salovich, SC Smith, M Cheung, RM Gerding…

Index: Emmitte, Kyle A.; Wilson, Brian J.; Baum, Erich W.; Emerson, Holly K.; Kuntz, Kevin W.; Nailor, Kristen E.; Salovich, James M.; Smith, Stephon C.; Cheung, Mui; Gerding, Roseanne M.; Stevens, Kirk L.; Uehling, David E.; Mook Jr., Robert A.; Moorthy, Ganesh S.; Dickerson, Scott H.; Hassell, Anne M.; Anthony Leesnitzer; Shewchuk, Lisa M.; Groy, Arthur; Rowand, Jason L.; Anderson, Kelly; Atkins, Charity L.; Yang, Jingsong; Sabbatini, Peter; Kumar, Rakesh Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 1004 - 1008

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Citation Number: 20

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.