1009941-01-8Relevant academic research and scientific papers
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK
Hom, Roy K.,Bowers, Simeon,Sealy, Jennifer M.,Truong, Anh P.,Probst, Gary D.,Neitzel, Martin L.,Neitz, R. Jeffrey,Fang, Larry,Brogley, Louis,Wu, Jing,Konradi, Andrei W.,Sham, Hing L.,Tóth, Gergely,Pan, Hu,Yao, Nanhua,Artis, Dean R.,Quinn, Kevin,Sauer, John-Michael,Powell, Kyle,Ren, Zhao,Bard, Frédérique,Yednock, Ted A.,Griswold-Prenner, Irene
, p. 7303 - 7307 (2010)
From high throughput screening, we discovered compound 1, the prototype for a series of disubstituted thiophene inhibitors of JNK which is selective towards closely related MAP kinases p38 and Erk2. Herein we describe the evolution of these compounds to a novel class of thiophene and thiazole JNK inhibitors that retain favorable solubility, permeability, and P-gp properties for development as CNS agents for treatment of neurodegeneration. Compound 61 demonstrated JNK3 IC50 = 77 nM and retained the excellent broad kinase selectivity observed for the series.
