Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
2010
Abstract 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 IC 50 = 77 nM and retained the excellent broad kinase selectivity observed for the series.
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