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

被引：42

作者：

Chaulet, Charlotte ^{[1
]}

Croix, Cecile ^{[1
]}

Alagille, David ^{[1
]}

Normand, Sylvain ^{[2
,3
]}

Delwail, Adriana ^{[2
,3
]}

Favot, Laure ^{[2
,3
]}

Lecron, Jean-Claude ^{[2
,3
]}

Viaud-Massuard, Marie-Claude ^{[1
]}

机构：

[1] Univ Tours, CNRS, UMR GICC Genet Immunotherapie Chim & Canc 6239, Equipe 5,Lab Chim Organ & Therapeut, F-37041 Tours, France

[2] Univ Poitiers, Lab Inflammat Tissus Epitheliaux & Cytokines EA 4, Poitiers, France

[3] CHU Poitiers Pole Biol Sante, Serv Immunol & Inflammat, Poitiers, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 03期

关键词：

Thalidomide; TNF-alpha; IL-6; 1H-Imidazo[1,5-a]indole-dione; Dihydro-thiadiazolo[2,3-b]-isoquinolinone-dioxide; 1H-Pyrrolo-[2,3-b]pyridine; NECROSIS-FACTOR-ALPHA; CONGENITAL ABNORMALITIES; DERIVATIVES;

D O I：

10.1016/j.bmcl.2010.12.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1019 / 1022

页数：4

共 17 条

[1] Timeline - The evolution of thalidomide and its IMiD derivatives as anticancer agents [J].