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Merck
CN

Pyridinylimidazole inhibitors of Tie2 kinase.

Bioorganic & medicinal chemistry letters (2007-07-10)
Marcus Semones, Yanhong Feng, Neil Johnson, Jerry L Adams, Jim Winkler, Michael Hansbury
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.