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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
; ; ; and
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
additional info
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)
id
58dd5e7f-04eb-4872-b723-950f7f7c215f (old id 1191569)
date added to LUP
2016-04-01 11:37:57
date last changed
2022-01-26 07:54:18
@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}},
  keywords     = {{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}},
  doi          = {{10.1016/j.bmc.2007.10.074}},
  volume       = {{16}},
  year         = {{2008}},
}