Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.

Journal Article (Journal Article)

The SAR of C5' functional groups with terminal basic amines at the C6 aniline of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines is reported. Examples demonstrate potent inhibition of IGF-1R with 1000-fold selectivity over JNK1 and 3 in enzymatic assays.

Full Text

Duke Authors

Cited Authors

  • Chamberlain, SD; Redman, AM; Wilson, JW; Deanda, F; Shotwell, JB; Gerding, R; Lei, H; Yang, B; Stevens, KL; Hassell, AM; Shewchuk, LM; Leesnitzer, MA; Smith, JL; Sabbatini, P; Atkins, C; Groy, A; Rowand, JL; Kumar, R; Mook, RA; Moorthy, G; Patnaik, S

Published Date

  • January 15, 2009

Published In

Volume / Issue

  • 19 / 2

Start / End Page

  • 360 - 364

PubMed ID

  • 19071018

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2008.11.077


  • eng

Conference Location

  • England