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

Summary, in English

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.

• Författare: Jan Rether; Gerhard Erkel; Timm Anke; Johan Eriksson Bajtner; Olov Sterner
• Avdelning/ar: Centrum för analys och syntes
• Publiceringsår: 2008
• Språk: Engelska
• Sidor: 1236-1241
• Publikation/Tidskrift/Serie: Bioorganic & Medicinal Chemistry
• Volym: 16
• Issue: 3
• Länkar: http://dx.doi.org/10.1016/j.bmc.2007.10.074
• Dokumenttyp: Artikel i tidskrift
• Förlag: Elsevier
• Ämne: Organic Chemistry
• Nyckelord: Semisynthesis; Podoscyphic acid; Inflammation; Promoter activity; TNF-α; Inhibitor
• Status: Published
• ISBN/ISSN/Övrigt: ISSN: 0968-0896