Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IκB kinase

James Kempson, Junqing Guo, Jagabandhu Das, Robert V. Moquin, Steven H. Spergel, Scott H. Watterson, Charles M. Langevine, Alaric J. Dyckman, Mark Pattoli, James R. Burke, Xiao Xia Yang, Kathleen M. Gillooly, Kim W. McIntyre, Laishun Chen, John Harold Dodd, Murray McKinnon, Joel C. Barrish, William J. Pitts

Research output: Contribution to journalArticlepeer-review

20 Scopus citations

Abstract

A new series of tricyclic-based inhibitors of IKK have been derived from an earlier lead compound. The synthesis and structure-activity relationships (SAR) are described. Compound 4k inhibited TNF production in rats stimulated with LPS.

Original languageEnglish (US)
Pages (from-to)2646-2649
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number10
DOIs
StatePublished - May 15 2009

All Science Journal Classification (ASJC) codes

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

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