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New Cyclams and their Copper(II) and Iron(III) Complexes: Synthesis and Potential Application as Anticancer Agents.

ChemMedChem 2019 January 30
New cyclam derivatives (HOCH2CH2CH2)2(PhCH2)2Cyclam and (HOCH2CH2CH2)2(4-CF3PhCH2)2Cyclam as well as their Cu(II) and Fe(III) complexes were synthesised and characterized and their stability in cellular media was assessed. The cytotoxic effect of all the compounds was examined on human cervical cancer cells (HeLa) revealing strong anticancer activity. After 24 h, only complexes bearing the (HOCH2CH2CH2)2(4-CF3PhCH2)2Cyclam ligand are cytotoxic, while at 72 h incubation all the compounds show significant antiproliferative effects. Notably, compounds containing 4-CF3PhCH2 pending arms on the cyclam ring revealed to be the most active with cytotoxicity values up to 12 times higher than cisplatin. All metal-complexes seem to induce cell death through ROS formation.

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