111883-52-4Relevant academic research and scientific papers
ANTIPARASITIC COMPOUNDS
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Page/Page column 52; 53, (2016/11/28)
The invention relates to thiazole derivatives and their use to treat parasites.
Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain
Sawyer, J. Scott,Beight, Douglas W.,Britt, Karen S.,Anderson, Bryan D.,Campbell, Robert M.,Goodson Jr., Theodore,Herron, David K.,Li, Hong-Yu,McMillen, William T.,Mort, Nicholas,Parsons, Stephen,Smith, Edward C. R.,Wagner, Jill R.,Yan, Lei,Zhang, Faming,Yingling, Jonathan M.
, p. 3581 - 3584 (2007/10/03)
We have expanded our previously reported series of pyrazole-based inhibitors of the TGF-β type I receptor kinase domain (TβR-I) to now include new 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole analogues. Limited examination of the SAR of this new series in both e
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain
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.
, p. 3953 - 3956 (2007/10/03)
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.
