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Structural-activity relationship study of highly-functionalized imidazolines as potent inhibitors of nuclear transcription factor-kappaB mediated IL-6 production.

Abstract：

:We herein describe the synthesis and anti-inflammatory properties of a small library of imidazoline-based NF-kappaB inhibitors. The structure-activity relationship of various substituents on an imidazoline core structure was evaluated for the ability to inhibit NF-kappaB mediated IL-6 production. Optimization of the scaffolds was pursued by correlating luciferase-based NF-kappaB reporter assays with inhibition of IL-6 production in IL-1beta stimulated human blood. Several derivatives were found to inhibit NF-kappaB mediated IL-6 production in the nanomolar range in IL-1beta stimulated human blood.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kahlon DK,Lansdell TA,Fisk JS,Tepe JJ

doi

10.1016/j.bmc.2009.03.002

subject

Has Abstract

pub_date

2009-04-15 00:00:00

pages

3093-103

issue

8

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00220-X

journal_volume

17

pub_type

杂志文章

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