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

Abstract:

AIM: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.

journal_name

Anticancer Res

journal_title

Anticancer research

authors

Ma X,Wu YI,Yang X,Yang S,Li Y,Huang Y,Lee RJ,Bai T,Luo Y

subject

Has Abstract

pub_date

2016-05-01 00:00:00

pages

2105-11

issue

5

eissn

0250-7005

issn

1791-7530

pii

36/5/2105

journal_volume

36

pub_type

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