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

Rether, Jan; Erkel, Gerhard; Anke, Timm; Eriksson Bajtner, Johan LU and Sterner, Olov LU (2008) In Bioorganic & Medicinal Chemistry 16(3). p.1236-1241
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.
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Semisynthesis, Podoscyphic acid, Inflammation, Promoter activity, TNF-α, Inhibitor
in
Bioorganic & Medicinal Chemistry
volume
16
issue
3
pages
1236 - 1241
publisher
Elsevier
external identifiers
  • wos:000253720100017
  • scopus:38849100378
ISSN
0968-0896
DOI
10.1016/j.bmc.2007.10.074
language
English
LU publication?
yes
id
58dd5e7f-04eb-4872-b723-950f7f7c215f (old id 1191569)
date added to LUP
2008-09-05 10:48:41
date last changed
2017-07-30 03:31:49
@article{58dd5e7f-04eb-4872-b723-950f7f7c215f,
  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.},
  author       = {Rether, Jan and Erkel, Gerhard and Anke, Timm and Eriksson Bajtner, Johan and Sterner, Olov},
  issn         = {0968-0896},
  keyword      = {Semisynthesis,Podoscyphic acid,Inflammation,Promoter activity,TNF-α,Inhibitor},
  language     = {eng},
  number       = {3},
  pages        = {1236--1241},
  publisher    = {Elsevier},
  series       = {Bioorganic & Medicinal Chemistry},
  title        = {Imidazo[1,2-a]pyridine derivatives as inhibitors of TNF-alpha expression in T cells},
  url          = {http://dx.doi.org/10.1016/j.bmc.2007.10.074},
  volume       = {16},
  year         = {2008},
}