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.

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Dyckman, AJ; Langevine, CM; Quesnelle, C; Kempson, J; Guo, J; Gill, P; Spergel, SH; Watterson, SH; Li, T; Nirschl, DS; Gillooly, KM; Pattoli, MA; McIntyre, KW; Chen, L; McKinnon, M; Dodd, JH; Barrish, JC; Burke, JR; Pitts, WJ

Published Date

  • January 1, 2011

Published In

Volume / Issue

  • 21 / 1

Start / End Page

  • 383 - 386

PubMed ID

  • 21087862

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2010.10.133


  • eng

Conference Location

  • England