Novel flavaglines displaying improved cytotoxicity.
Fiche publication
Date publication
janvier 2011
Auteurs
Membres identifiés du Cancéropôle Est :
Dr DESAUBRY Laurent, Dr GAIDDON Christian
Tous les auteurs :
Thuaud F, Ribeiro N, Gaiddon C, Cresteil T, Desaubry L
Lien Pubmed
Résumé
Novel flavagline analogues were synthesized and examined with respect to their cytotoxicity. Structural features critical to the potential of this class of anticancer natural products were unraveled. We demonstrated, in particular, that the introduction of substituants at C-2 has a deleterious effect on multidrug resistance. Replacement of the hydroxy at C-1 by an aminoformyl with the opposite configuration enhances the cytotoxicity and led to a compound that reduces tumors growth in an allograft model at nontoxic doses.
Référence
J Med Chem. 2011 Jan 13;54(1):411-5