1. Design, synthesis and biological evaluation of new thalidomide analogues as TNF-α and IL-6 production inhibitors
- Author
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Cécile Croix, Marie-Claude Viaud-Massuard, David Alagille, Adriana Delwail, Sylvain Normand, Laure Favot, Charlotte Chaulet, Jean-Claude Lecron, Génétique, immunothérapie, chimie et cancer (GICC), UMR 6239 CNRS [2008-2011] (GICC UMR 6239 CNRS), Université de Tours-Centre National de la Recherche Scientifique (CNRS), Laboratoire Inflammation, Tissus épithéliaux et Cytokines (LITEC), Université de Poitiers, and Université de Tours (UT)-Centre National de la Recherche Scientifique (CNRS)
- Subjects
medicine.medical_treatment ,Clinical Biochemistry ,Pharmaceutical Science ,Down-Regulation ,[CHIM.THER]Chemical Sciences/Medicinal Chemistry ,Pharmacology ,01 natural sciences ,Biochemistry ,Peripheral blood mononuclear cell ,03 medical and health sciences ,0302 clinical medicine ,Downregulation and upregulation ,1H-Imidazo[1 ,5-a]indole-dione ,Drug Discovery ,medicine ,Humans ,Interleukin 6 ,Molecular Biology ,Lenalidomide ,IL-6 ,3-b]pyridine ,biology ,010405 organic chemistry ,Chemistry ,Interleukin-6 ,Tumor Necrosis Factor-alpha ,Organic Chemistry ,Interleukin ,1H-Pyrrolo-[2 ,Dihydro-thiadiazolo[2 ,3-b]-isoquinolinone-dioxide ,3. Good health ,0104 chemical sciences ,Thalidomide ,Cytokine ,030220 oncology & carcinogenesis ,Drug Design ,biology.protein ,Leukocytes, Mononuclear ,Molecular Medicine ,Tumor necrosis factor alpha ,TNF-alpha ,medicine.drug - Abstract
International audience; 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)-alpha 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-alpha and IL-6 production. (C) 2010 Elsevier Ltd. All rights reserved.
- Published
- 2010
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