2. Academic Validation
  3. Pyridinylimidazole inhibitors of Tie2 kinase

Pyridinylimidazole inhibitors of Tie2 kinase

  • Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60. doi: 10.1016/j.bmcl.2007.06.068.
Marcus Semones 1,  Yanhong Feng,  Neil Johnson,  Jerry L Adams,  Jim Winkler,  Michael Hansbury
Affiliations

Affiliation

  • 1 GlaxoSmithKline, Collegeville, PA 19426, USA. marcus.a.semones@gsk.com
PMID: 17618114 DOI: 10.1016/j.bmcl.2007.06.068
Abstract

This communication details the evolution of the screening lead SB-203580, a known CSBP/p38 kinase inhibitor, into a potent and selective Tie2 tyrosine kinase inhibitor. The optimized compound 5 showed efficacy in an in vivo model of angiogenesis and a MOPC-315 plasmacytoma xenograft model.

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