2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133.
Alaric J Dyckman 1,  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
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb, Research and Development, Princeton, NJ 08543-4000, USA. alaric.dyckman@bms.com
PMID: 21087862 DOI: 10.1016/j.bmcl.2010.10.133
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.

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