3481-90-1Relevant academic research and scientific papers
Mesoions and ketene valence isomers. Pyrrolo[1,2-a]pyridinylium olates and (2-pyridyl)carbonylketenes
Ye, Xuan,Andraos, John,Bibas, Herve,Wong, Ming Wah,Wentrup, Curt
, p. 401 - 406 (2000)
The synthesis and isolation of the pyrrolopyridinium olate system was discussed. The zwitterionic compounds were obtained by flash vacuum thermolysis (FVT) of picolinoylacetates. Nucleophilic addition reactions of zwitterionic compounds occurred by C-N bond cleavage to afford pyridine derivatives. The kinetic monitoring of such reactions revealed that they have extremely low activation enthalpies and very large negative activation entropies.
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.
