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

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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; Sterner, Olov.

In: Bioorganic & Medicinal Chemistry, Vol. 16, No. 3, 2008, p. 1236-1241.

Research output: Contribution to journalArticle

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Rether, Jan ; Erkel, Gerhard ; Anke, Timm ; Eriksson Bajtner, Johan ; Sterner, Olov. / Imidazo[1,2-a]pyridine derivatives as inhibitors of TNF-alpha expression in T cells. In: Bioorganic & Medicinal Chemistry. 2008 ; Vol. 16, No. 3. pp. 1236-1241.

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TY - JOUR

T1 - Imidazo[1,2-a]pyridine derivatives as inhibitors of TNF-alpha expression in T cells

AU - Rether, Jan

AU - Erkel, Gerhard

AU - Anke, Timm

AU - Eriksson Bajtner, Johan

AU - Sterner, Olov

N1 - 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)

PY - 2008

Y1 - 2008

N2 - 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.

AB - 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.

KW - Semisynthesis

KW - Podoscyphic acid

KW - Inflammation

KW - Promoter activity

KW - TNF-α

KW - Inhibitor

U2 - 10.1016/j.bmc.2007.10.074

DO - 10.1016/j.bmc.2007.10.074

M3 - Article

VL - 16

SP - 1236

EP - 1241

JO - Bioorganic and Medicinal Chemistry

T2 - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

SN - 0968-0896

IS - 3

ER -