39697-33-1Relevant academic research and scientific papers
Bioisosteric Replacement of Arylamide-Linked Spine Residues with N-Acylhydrazones and Selenophenes as a Design Strategy to Novel Dibenzosuberone Derivatives as Type i 1/2 p38α MAP Kinase Inhibitors
Pedreira, Júlia G. B.,Nahidino, Philipp,Kudolo, Mark,Pantsar, Tatu,Berger, Benedict-Tilman,Forster, Michael,Knapp, Stefan,Laufer, Stefan,Barreiro, Eliezer J.
, p. 7347 - 7354 (2020/09/11)
The recent disclosure of type I 1/2 inhibitors for p38α MAPK demonstrated how the stabilization of the R-spine can be used as a strategy to greatly increase the target residence time (TRT) of inhibitors. Herein, for the first time, we describe N-acylhydrazone and selenophene residues as spine motifs, yielding metabolically stable inhibitors with high potency on enzymatic, NanoBRET, and whole blood assays, improved metabolic stability, and prolonged TRT.
