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Literature DB >> 21215621

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

Charlotte Chaulet¹, Cécile Croix, David Alagille, Sylvain Normand, Adriana Delwail, Laure Favot, Jean-Claude Lecron, Marie-Claude Viaud-Massuard.

Abstract

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.

Entities: Chemical Gene

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Year: 2010 PMID： 21215621 DOI： 10.1016/j.bmcl.2010.12.031

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

6 in total

1. Responsiveness of cytogenetically discrete human myeloma cell lines to lenalidomide: lack of correlation with cereblon and interferon regulatory factor 4 expression levels.

Authors: Alexandra J Greenberg; Denise K Walters; Shaji K Kumar; S Vincent Rajkumar; Diane F Jelinek
Journal: Eur J Haematol Date: 2013-09-17 Impact factor: 2.997

2. Design, synthesis and biological assessment of novel N-substituted 3-(phthalimidin-2-yl)-2,6-dioxopiperidines and 3-substituted 2,6-dioxopiperidines for TNF-α inhibitory activity.

Authors: Weiming Luo; Qian-sheng Yu; Isidro Salcedo; Harold W Holloway; Debomoy K Lahiri; Arnold Brossi; David Tweedie; Nigel H Greig
Journal: Bioorg Med Chem Date: 2011-05-23 Impact factor: 3.641

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

1. Responsiveness of cytogenetically discrete human myeloma cell lines to lenalidomide: lack of correlation with cereblon and interferon regulatory factor 4 expression levels.

2. Design, synthesis and biological assessment of novel N-substituted 3-(phthalimidin-2-yl)-2,6-dioxopiperidines and 3-substituted 2,6-dioxopiperidines for TNF-α inhibitory activity.

3. Novel targeted treatment strategies for refractory chronic lymphocytic leukaemia.

Review 4. Mechanism of immunomodulatory drugs' action in the treatment of multiple myeloma.

5. Lenalidomide overcomes the immunosuppression of regulatory CD8⁺CD28^- T-cells.

Review 6. E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points.

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

1. Responsiveness of cytogenetically discrete human myeloma cell lines to lenalidomide: lack of correlation with cereblon and interferon regulatory factor 4 expression levels.

2. Design, synthesis and biological assessment of novel N-substituted 3-(phthalimidin-2-yl)-2,6-dioxopiperidines and 3-substituted 2,6-dioxopiperidines for TNF-α inhibitory activity.

3. Novel targeted treatment strategies for refractory chronic lymphocytic leukaemia.

Review 4. Mechanism of immunomodulatory drugs' action in the treatment of multiple myeloma.

5. Lenalidomide overcomes the immunosuppression of regulatory CD8+CD28- T-cells.

Review 6. E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points.

5. Lenalidomide overcomes the immunosuppression of regulatory CD8⁺CD28^- T-cells.