Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain
Journal of Medicinal Chemistry2003Vol. 46(19), pp. 3953–3956
Citations Over TimeTop 10% of 2003 papers
J. Scott Sawyer, Bryan D. Anderson, Douglas W. Beight, Robert M. Campbell, Michael L. Jones, David K. Herron, John W. Lampe, Jefferson R. McCowan, William T. McMillen, Nicholas Mort, Stephen H. Parsons, Edward C. Smith, Michal Vieth, Leonard C. Weir, Lei Yan, Faming Zhang, Jonathan M. Yingling
Abstract
Pyrazole-based inhibitors of the transforming growth factor-beta type I receptor kinase domain (TbetaR-I) are described. Examination of the SAR in both enzyme- and cell-based in vitro assays resulted in the emergence of two subseries featuring differing selectivity versus p38 MAP kinase. A common binding mode at the active site has been established by successful cocrystallization and X-ray analysis of potent inhibitors with the TbetaR-I receptor kinase domain.
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