Anchoring and bola cationic amphiphiles for nucleotide delivery. Effects of orientation and extension of hydrophobic regions

Novel cationic amphiphiles, based on lithocholic acid derivatives with two structural motifs, anchoring lipids and bola lipids, were designed and synthesized. Both bear extended hydrophobic space-filling substituents. A significant effect of the orientation and extension of hydrophobic regions around the ether linkage at the 3-position was found on the efficiency of DNA delivery. (C) 2001 Elsevier Science Ltd. All rights reserved.