A novel 2,4-diaminopyrimidine derivative as selective inhibitor of protein kinase C theta prevents allograft rejection in a rat heart transplant model

Add time:07/17/2019    Source:sciencedirect.com

Protein kinase C theta (PKCθ) plays a critical role in T cell signaling and is an attractive target for the treatment of T cell-mediated diseases such as transplant rejection and autoimmune disease. To identify PKCθ inhibitors, we focused on the 2,6-diamino-3-carbamoyl-5-cyanopyrazine derivative 2, which exhibited moderate PKCθ inhibitory activity. Optimization of 2 identified the 2,4-diamino-5-cyanopyrimidine derivative 16c, which exhibited potent PKCθ inhibitory activity and showed good selectivity against other PKC isozymes. Compound 16c prolonged graft survival in an in vivo rat heterotopic cardiac transplant model.

We also recommend Trading Suppliers and Manufacturers of 2,4-DICHLORO-5-(TRIFLUOROMETHOXY)ANILINE (cas 1598-42-1). Pls Click Website Link as below: cas 1598-42-1 suppliers

Prev:Novel highly selective fluorescent sensor based on electrosynthesized poly(9-fluorenecarboxylic acid) for efficient and practical detection of iron(III) and its agricultural application
Next:Homolytic substitution at selenium: ring closure of ω-(benzylseleno)alkyl radicals)