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The ability of non-viral gene delivery systems to overcome extracellular and intracellular barriers is a critical issue for future clinical applications of gene therapy. In recent years much effort has been focused on the development of a variety of DNA carriers, and cationic liposomes have become the most common non-viral gene delivery system. Solid-phase synthesis was used to produce three libraries of polyamine-based cationic lipids with diverse hydrophobic tails. These were characterised, and structure-activity relationships were determined for DNA binding and transfection ability of these compounds when formulated as cationic liposomes. Two of the cationic lipids produced high-efficiency transfection of human cells. Surprisingly, these two compounds were from the library with two headgroups and one aliphatic tail, a compound class regarded as detergent-like and little investigated for transfection. These cationic lipids are promising reagents for gene delivery and illustrate the potential of solid-phase synthesis methods for lipoplex discovery.

Original publication




Journal article


Chemistry (Weinheim an der Bergstrasse, Germany)

Publication Date





463 - 473


Department of Chemistry, University of Southampton, Southampton SO17 1BJ, UK.


Cell Line, Humans, Cations, Guanidine, Polyamines, Lipids, DNA, Transfection, Cell Survival, Binding Sites, Molecular Structure, Structure-Activity Relationship, Genetic Vectors, Plasmids