Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Published
Journal Article
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.
Full Text
Duke Authors
Cited Authors
- 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
Published Date
- February 1, 2009
Published In
Volume / Issue
- 19 / 3
Start / End Page
- 1004 - 1008
PubMed ID
- 19101143
Pubmed Central ID
- 19101143
Electronic International Standard Serial Number (EISSN)
- 1464-3405
Digital Object Identifier (DOI)
- 10.1016/j.bmcl.2008.11.058
Language
- eng
Conference Location
- England