Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
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.
Emmitte, KA; Wilson, BJ; Baum, EW; Emerson, HK; Kuntz, KW; Nailor, KE; Salovich, JM; Smith, SC; Cheung, M; Gerding, RM; Stevens, KL; Uehling, DE; Mook, RA; Moorthy, GS; Dickerson, SH; Hassell, AM; Leesnitzer, MA; Shewchuk, LM; Groy, A; Rowand, JL; Anderson, K; Atkins, CL; Yang, J; Sabbatini, P; Kumar, R
Volume / Issue
Start / End Page
Electronic International Standard Serial Number (EISSN)
Digital Object Identifier (DOI)