Imidazo[1,2-a]pyridine derivatives as inhibitors of TNF-alpha expression in T cells

Research output: Contribution to journalArticle

Abstract

Novel hexahydroimidazo[1,2-a]pyridines prepared by the addition of ethyl (1-benzylimidazolidin-2-ylidene)acetate (2) to the fungal metabolite podoscyphic acid (1a) and esters of 1a have been evaluated for their ability to inhibit the inducible TNF-α promoter activity in T cells. The methyl ester 3b is the most potent, inhibiting the TNF-α driven reporter gene expression in Jurkat T cells with an IC50-value of 2.0 μg/ml (3.6 μM). In addition, compound 3b inhibited the inducible TNF-α production in the myelomonocytic U937 cells with an IC50-value of 4.6 μM.

Details

Authors
  • Jan Rether
  • Gerhard Erkel
  • Timm Anke
  • Johan Eriksson Bajtner
  • Olov Sterner
Organisations
Research areas and keywords

Subject classification (UKÄ) – MANDATORY

  • Organic Chemistry

Keywords

  • Semisynthesis, Podoscyphic acid, Inflammation, Promoter activity, TNF-α, Inhibitor
Original languageEnglish
Pages (from-to)1236-1241
JournalBioorganic & Medicinal Chemistry
Volume16
Issue number3
Publication statusPublished - 2008
Publication categoryResearch
Peer-reviewedYes

Bibliographic note

The information about affiliations in this record was updated in December 2015. The record was previously connected to the following departments: Organic chemistry (S/LTH) (011001240)