Synthesis and preliminary biological studies of hemifluorinated bifunctional bolaamphiphiles designed for gene delivery
The multistep synthesis of a new series of dissymmetric hemifluorocarbon bolaamphiphiles designed for gene transport is described. The dissymmetric functionalization of diiodoperfluoroctane leads to bolaamphiphile molecules composed of a partially fluorocarbon core end-capped with a glycoside and an ammonium salt derived from histidine or lysine. Initial biological results indicate that one of the bolaamphiphile - end-capped with a lysine and a lactobionamide residue - induces a remarkably low cytotoxicity on COS-7 cells and, when self-assembled with DNA plasmid, generates a significant in vitro transfection efficiency without the addition of any fusogenic lipid. the Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2006.
Denoyelle, Severine,Polidori, Ange,Brunelle, Melanie,Vuillaume, Pascal Y.,Laurent, Sylvette,ElAzhary, Yousef,Pucci, Bernard
p. 629 - 646
(2007/10/03)
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