Please use this identifier to cite or link to this item: http://hdl.handle.net/1959.13/922289

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Title
Substituted 9-aminoacridine-4-carboxamides tethered to platinum(II)diamine complexes: Chemistry, cytotoxicity and DNA sequence selectivity
Author/Creator
Carland, Michael;  Grannas, Martin J.;  Cairns, Murray J.;  Roknic, Vanessa J.;  Denny, William A.;  McFadyen, W. David;  Murray, Vincent
Institution
The University of Newcastle. Faculty of Health, School of Biomedical Sciences and Pharmacy
Description
Three platinum complexes in which substituted (7-OMe, 9-NH₂; 7-F, 9-NH₂; and 7-H, 9-NH(CH₂)₂OH) 9-aminoacridine-4-carboxamides were tethered to a platinum(II)diamine moiety were synthesised and characterised at the chemical and biological level. These variants showed a decrease in cytotoxicity, as measured by IC₅₀ values in HeLa cells, when compared with the parent 7-H, 9-NH₂ compound. The 7-F and 9-NH(CH₂)₂OH substituents gave rise to a small decrease in cytotoxicity, and the 7-OMe substituent resulted in a larger decrease in cytotoxicity. Their binding to purified pUC19 plasmid DNA was investigated and it was found that the addition of 7-F, 9-NH(CH₂)₂OH and especially the 7-OMe substituents, resulted in reduced DNA binding. This correlated well with the IC₅₀ cytotoxicity values. However, the DNA sequence selectivity was unaffected by the addition of these moieties.
Relation
Journal of Inorganic Biochemistry Vol. 104, Issue 8, p. 815-819
Publisher Link
http://dx.doi.org/10.1016/j.jinorgbio.2010.03.011
Date
2010
Publisher
Elsevier
Keyword(s)
acridine-4-carboxamides;  substituents;  platinum(II);  synthesis;  cytotoxicity;  DNA sequence selectivity
Resource Type
journal article
Identifier
http://hdl.handle.net/1959.13/922289
Identifier
ISSN:0162-0134
Reviewed
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Subject
"Journal of Inorganic Biochemistry"
 
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