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An Investigation of the DNA Interactions of Polyamine Anthracene Conjugates under High Ionic Conditions

Six polyamine anthracene conjugates (Ants) were studied that take advantage of the polyamine transporter system (PTS) to target specific cancer. The structural features of the Ants involve planar aromatic anthracene that has highly cytotoxicity properties and a polyamine chain similar to natural polyamine, which is taken up by eukaryote cells expressing the PTS actively. Experimental data show that Ants with di-substituted polyamine chains have significantly higher DNA binding affinities than the mono-substituted anthracene conjugates. The high ionic conditions (~150 mM NaCl and 260 mM KCl) in the eukaryote cell nucleus extensively impair the apparent DNA binding of the Ants, but may further reinforce DNA structural stability. Combining the published cytotoxicity of the PTS data with the DNA interaction data reported here, the di-substituted polyamine anthracene conjugates have the highest potential to, after cellular uptake via PTS, bind to DNA.

Identiferoai:union.ndltd.org:GEORGIA/oai:scholarworks.gsu.edu:chemistry_theses-1096
Date14 December 2016
CreatorsNguyen, Khoa
PublisherScholarWorks @ Georgia State University
Source SetsGeorgia State University
Detected LanguageEnglish
Typetext
Formatapplication/pdf
SourceChemistry Theses

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