期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 13, 页码 4056-4063出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.05.007
关键词
Drug delivery systems; Cancer therapy; Controlled release; Acridines; Hydrazone
资金
- Grant Agency of the Academy of Sciences of the Czech Republic [IAAX00500803]
- Grant Agency of the Czech Republic [P207/10/P054]
Acridines are potent DNA-intercalating anticancer agents with high in vivo anticancer effectiveness, but also severe side effects. We synthesized five 9-anilinoacridine-type drugs and their conjugates with biocompatible water-soluble hydrazide polymer carrier. All of the synthesized acridine drugs retained their in vitro antiproliferative properties. Their polymer conjugates were sufficiently stable at pH 7.4 (model of pH in blood plasma) while releasing free drugs at pH 5.0 (model of pH in endosomes). After internalization of the conjugates, the free drugs were released and are visible in cell nuclei by fluorescence microscopy. Their intercalation ability was proven using a competitive ethidium bromide displacement assay. (C) 2012 Elsevier Ltd. All rights reserved.
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