کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358597 | 981350 | 2012 | 8 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Polymer conjugates of acridine-type anticancer drugs with pH-controlled activation Polymer conjugates of acridine-type anticancer drugs with pH-controlled activation](/preview/png/1358597.png)
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.
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Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 13, 1 July 2012, Pages 4056–4063