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
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- 作者：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. P
- 关键词：IKK ; IKK2 ; IKKβ ; NF-κ ; B
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2011
- 出版时间：1 January 2011
- 年：2011
- 卷：21
- 期：1
- 页码：383-386
- 全文大小：1594 K
文摘
The synthesis, structure–activity relationships (SAR) and biological evaluation of thiazole based tricyclic inhibitors of IKK2 are described. Compound 9 was determined to be orally efficacious in a murine model of rheumatoid arthritis.