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DNA binding and antiproliferative activity of copper (II) complexes of Quinolone‐thiazole derivatives with applications as a chemotherapeutic agent
Author(s) -
Foreman David Rudolph,
Lin Han Xing,
Fox Kristin M.,
Tanski Joseph M,
Tyler Laurie A.
Publication year - 2013
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.27.1_supplement.801.2
Subject(s) - ethidium bromide , nuclease , chemistry , thiazole , copper , dna , combinatorial chemistry , cisplatin , ligand (biochemistry) , bromide , stereochemistry , biochemistry , inorganic chemistry , organic chemistry , biology , receptor , chemotherapy , genetics
Transition metal based complexes that exhibit nuclease activity have garnered interest due to their chemotherapeutic applications. Cisplatin has been regarded as one of the most effective drugs, however toxicities and drug resistance has limited its clinical use. Copper (II) centered complexes are promising due to the importance of copper for a range of physiological processes, including enzyme and protein activity. Copper is also found in high concentrations in tumor cells as it is needed for angiogenesis. We have synthesized and characterized several copper complexes that are derived from a thiazole ligand backbone that express nuclease activity: [Cu(8OHQ(oBt))Cl2] and [Cu(8OQ)(oBt))Cl(MeOH)]. These complexes contain step‐wise structural modifications allowing structure function comparisons to be made. DNA cleavage and binding studies were carried out using gel electrophoresis, ethidium bromide, and UV‐Vis Spectroscopy. Quantitative analyses from each of the above studies were used to assess nuclease efficiency, binding efficiency and the copper compounds’ interaction with DNA and BSA.