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Design, synthesis and biological evaluation of new thalidomide analogues as TNF-α and IL-6 production inhibitors

✍ Scribed by Charlotte Chaulet; Cécile Croix; David Alagille; Sylvain Normand; Adriana Delwail; Laure Favot; Jean-Claude Lecron; Marie-Claude Viaud-Massuard

Publisher: Elsevier Science
Year: 2011
Tongue: English
Weight: 620 KB
Volume: 21
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.12.031

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✦ Synopsis

Several thalidomide analogues were synthesized and compared to thalidomide and its more active analogue, lenalidomide, for their ability to inhibit the production of the pro-inflammatory cytokine tumour necrosis factor (TNF)-α and interleukin (IL)-6 by LPS-activated peripheral blood mononuclear cells (PBMCs). Among these compounds, two analogues containing sulfonyl group displayed interesting downregulation of TNF-α and IL-6 production.

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