A Novel 1,2-Dihydroquinoline Anticancer Agent and Its Delivery to Tumor Cells Using Cationic Liposomes

We screened nine 1,2-dihydro-quinolines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay in HepG2 and SMMC cells and identified ethyl-2-cyano-2-(2- (methoxycarbonyl)allyl)quinoline-1(2H)-carboxylate (compound 5) as a potential anticancer agent. In order to further develop its anticancer therapeutic potential, we incorporated this agent into cationic liposomes for delivery to tumor cells. The characteristics of liposomes, their cytotoxicity and cellular uptake by tumor cells were investigated. We demonstrated that cationic 1,2-dioleoyl-3- trimethyl-ammonium-propane containing liposomes (cLips) loaded with compound 5 has superior antitumor activity compared to neutral liposomes. These data suggest cLip-compound 5 to be a promising agent that warrants further evaluation.