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

Research output: Contribution to journalArticle

6 Scopus citations

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 orally efficacious in a murine model of rheumatoid arthritis.

Original languageEnglish (US)
Pages (from-to)383-386
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number1
DOIs
StatePublished - Jan 1 2011

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    Dyckman, A. J., Langevine, C. M., Quesnelle, C., Kempson, J., Guo, J., Gill, P., Spergel, S. H., Watterson, S. H., Li, T., Nirschl, D. S., Gillooly, K. M., Pattoli, M. A., McIntyre, K. W., Chen, L., McKinnon, M., Dodd, J. H., Barrish, J. C., Burke, J. R., & Pitts, W. J. (2011). 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. Bioorganic and Medicinal Chemistry Letters, 21(1), 383-386. https://doi.org/10.1016/j.bmcl.2010.10.133