Synthesis and activity of new aryl-and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain
JS Sawyer, BD Anderson, DW Beight… - Journal of medicinal …, 2003 - ACS Publications
JS Sawyer, BD Anderson, DW Beight, RM Campbell, ML Jones, DK Herron, JW Lampe…
Journal of medicinal chemistry, 2003•ACS PublicationsPyrazole-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.
(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.
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.
ACS Publications