Preliminary biological evaluations of new thalidomide analogues for multiple sclerosis application

Christiane Contino-Pépin; Audrey Parat; Sandrine Périno; Christine Lenoir; Michel Vidal; Hervé Galons; Stephen Karlik; Bernard Pucci

doi:10.1016/j.bmcl.2008.11.118

Preliminary biological evaluations of new thalidomide analogues for multiple sclerosis application

Bioorg Med Chem Lett. 2009 Feb 1;19(3):878-81. doi: 10.1016/j.bmcl.2008.11.118. Epub 2008 Dec 7.

Authors

Christiane Contino-Pépin¹, Audrey Parat, Sandrine Périno, Christine Lenoir, Michel Vidal, Hervé Galons, Stephen Karlik, Bernard Pucci

Affiliation

¹ Université d'Avignon, Laboratoire de Chimie Bioorganique et des Systèmes Moléculaires Vectoriels, 33 rue Louis Pasteur, 84000 Avignon, France. christine.pepin@univ-avignon.fr

PMID: 19103485
DOI: 10.1016/j.bmcl.2008.11.118

Abstract

The present work deals with the synthesis of a new series of thalidomide derivatives for therapeutic applications. These compounds were evaluated in vitro on a human endothelial cell line EA.hy926 for their antiproliferative potential and in vivo on an experimental animal multiple sclerosis model called EAE as angiogenesis inhibitors. The preliminary results obtained on EAE assays seem to validate that anti-angiogenesis compounds could be promising tools for the treatment of MS.

MeSH terms

Angiogenesis Inhibitors / chemical synthesis
Angiogenesis Inhibitors / pharmacology*
Animals
Cell Line
Cell Proliferation
Chemistry, Pharmaceutical / methods*
Drug Design
Encephalomyelitis, Autoimmune, Experimental / drug therapy*
Endothelial Cells / metabolism
Humans
Models, Chemical
Multiple Sclerosis / drug therapy*
Neovascularization, Pathologic
Thalidomide / analogs & derivatives*
Thalidomide / chemical synthesis
Thalidomide / pharmacology*

Substances

Angiogenesis Inhibitors
Thalidomide