Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK
Journal Article
·
· Bioorg. Med. Chem. Lett.
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{sub 50} = 77 nM and retained the excellent broad kinase selectivity observed for the series.
- Research Organization:
- Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
- Sponsoring Organization:
- USDOE Office of Science (SC)
- OSTI ID:
- 1026552
- Journal Information:
- Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (24) ; 12, 2010 Vol. 20
- Country of Publication:
- United States
- Language:
- ENGLISH
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