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Biological, Electrochemical and Spectroscopic Study of Cu (II) Complexes: Applications to the Development of Anticancer Metallodrugs
Author(s) -
Lewis Adam,
Fox Kristin,
Tanski Joseph,
Tyler Laurie
Publication year - 2016
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.30.1_supplement.842.1
Subject(s) - benzothiazole , chemistry , benzimidazole , human serum albumin , cyclic voltammetry , binding constant , combinatorial chemistry , pyridine , ligand (biochemistry) , redox , electrochemistry , quenching (fluorescence) , fluorescence , nuclear chemistry , chromatography , binding site , inorganic chemistry , medicinal chemistry , organic chemistry , biochemistry , physics , receptor , electrode , quantum mechanics
The activity of several Cu (II) complexes with three different biologically relevant ligand systems – benzimidazole, benzothiazole, or derivatized pyridine‐moieties – were assessed to determine structure‐function relationships important to the application of these complexes as anticancer agents. Topoisomerase I (Topo I) inhibition activity was evaluated by monitoring the complexes’ ability to prevent relaxation of supercoiled (SC) DNA via gel electrophoresis. Human Serum Albumin (HSA) binding ability was measured using a fluorescence quenching‐based assay. The Stern‐Volmer equation was then used to determine the binding constants for the complexes with HSA. The reduction potential for the Cu II/I redox couple for each complex was determined using cyclic voltammetry. The electrochemical and biological data will be discussed and related to the coordination sphere around the Cu(II).