Polymer conjugates of acridine-type anticancer drugs with pH-controlled activation

…, J Svoboda, D Kaňková, J Kovář, K Ulbrich

Index: Sedlacek, Ondrej; Hruby, Martin; Studenovsky, Martin; Vetvicka, David; Svoboda, Jan; Kankova, Dana; Kovar, Jan; Ulbrich, Karel Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 13 p. 4056 - 4063

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Citation Number: 21

Abstract

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 ...