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Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: Synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis

Alaric J. Dyckman,Charles M. Langevine,Claude Quesnelle,James Kempson,Junqing Guo,Patrice Gill,Steven H. Spergel,Scott H. Watterson,Tianle Li,David S. Nirschl,Kathleen M. Gillooly,Mark A. Pattoli,Kim W. McIntyre,Laishun Chen,Murray McKinnon,John H. Dodd,Joel C. Barrish,James R. Burke,William J. Pitts

Bioorganic & Medicinal Chemistry Letters（2011）

Cited 16|Views69
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Abstract
The synthesis, structure–activity relationships (SAR) and biological evaluation of thiazole based tricyclic inhibitors of IKK2 are described. Compound 9 was determined to be efficacious in a murine model for rheumatoid arthritis.
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Key words
IKK,IKK2,IKKβ,NF-κB
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