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Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain |
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| Authors: | Sawyer J Scott Anderson Bryan D Beight Douglas W Campbell Robert M Jones Michael L Herron David K Lampe John W McCowan Jefferson R McMillen William T Mort Nicholas Parsons Stephen Smith Edward C R Vieth Michal Weir Leonard C Yan Lei Zhang Faming Yingling Jonathan M |
| Affiliation: | Discovery Chemistry Research and Technology, The Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA. jss@lilly.com |
| 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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