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

Journal Article (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

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2008.11.058


  • eng

Conference Location

  • England