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
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 Parsons
Edward C. R. Smith
Michal Vieth
Leonard C. Weir
Lei Yan
Faming Zhang
Jonathan M. Yingling
10.1021/jm0205705.s001
https://acs.figshare.com/articles/journal_contribution/Synthesis_and_Activity_of_New_Aryl-_and_Heteroaryl-Substituted_Pyrazole_Inhibitors_of_the_Transforming_Growth_Factor-_Type_I_Receptor_Kinase_Domain/3681318
Pyrazole-based inhibitors of the transforming growth
factor-β type I receptor kinase domain (TβR-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 TβR-I receptor kinase domain.
2003-08-12 00:00:00
p 38 MAP kinase
T βR receptor kinase domain
T βR
SAR
binding mode
New Aryl
receptor kinase domain
inhibitor