761000-09-3Relevant academic research and scientific papers
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors
Townes, Jennifer A.,Golebiowski, Adam,Clark, Michael P.,Laufersweiler, Matthew J.,Brugel, Todd A.,Sabat, Mark,Bookland, Roger G.,Laughlin, Steve K.,VanRens, John C.,De, Biswanath,Hsieh, Lily C.,Xu, Susan C.,Janusz, Michael J.,Walter, Richard L.
, p. 4945 - 4948 (2004)
4-Aryl-5-pyrimidyl-based cytokine synthesis inhibitors of TNF-α production, which contain a novel bicyclic pyrazole heterocyclic core, are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-α production in a THP-1 cell-based assay and against human p38α MAP kinase in an isolated enzyme assay. The X-ray crystal structure of a bicyclic pyrazole inhibitor co-crystallized with mutated p38 (mp38) is presented. 4-Aryl-5-pyrimidyl-based cytokine synthesis inhibitors of TNF-α production, which contain a novel bicyclic pyrazole heterocyclic core, are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-α production in a THP-1 cell-based assay and against human p38α MAP kinase in an isolated enzyme assay. The X-ray crystal structure of a bicyclic pyrazole inhibitor co-crystallized with mutated p38 (mp38) is presented.
