Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain
J. Scott Sawyer(Eli Lilly (United States)), Bryan D. Anderson(Eli Lilly (United States)), Douglas W. Beight(Eli Lilly (United States)), Robert M. Campbell(Eli Lilly (United States)), Michael L. Jones(Eli Lilly (United States)), David K. Herron(Eli Lilly (United States)), John W. Lampe(Eli Lilly (United States)), Jefferson R. McCowan(Eli Lilly (United States)), William T. McMillen(Eli Lilly (United States)), Nicholas Mort(Eli Lilly (United States)), Stephen H. Parsons(Eli Lilly (United States)), Edward C. Smith(Eli Lilly (United States)), Michal Vieth(Eli Lilly (United States)), Leonard C. Weir(Eli Lilly (United States)), Lei Yan(Eli Lilly (United States)), Faming Zhang(Eli Lilly (United States)), Jonathan M. Yingling(Eli Lilly (United States))
Cited by 237Open Access
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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