The synthesis and characterization of a series of copper(II) complexes containing either a benzimidazole (BI) or a benzothiazole (BT) moitey within the ligand periphery are reported along with their comparative biological activity. The biological activity has been assessed by analyzing DNA interaction, nuclease ability, cytotoxic activity and antibacterial properties. Mechanistic studies indicate all complexes utilize an oxidative mechanism however the principal reactive oxygen species (ROS) is different; the BI containing complexes utilize O2- as the principal reactive oxygen species while the BT containing species utilize 1O2. Overall, the complexes contining a BT moiety in the ligand frame exhibit pronounced activity at lower concentrations compared to the BI derivities. The interaction between the complexes and DNA was investigated using fluorescence emission spectroscopy and revealed all complexes strongly intercalate DNA with Kapp values on the order of 106. The cytotoxic effects of the complexes were examined using HeLa and K562 cells and show cell death in the micromolar range. Similar reactivity was observed in the antibacterial studies with E. coli and S. aureus. A comparative analysis the complexes is presented.

Chemical biology of Cu(II) complexes with imidazole or thiazole containing ligands:  Synthesis, crystal structures and comparative biological activity

253rd National Meeting (2017)

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