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

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New cyclam derivatives (HOCH2CH2CH2)2(PhCH2)2Cyclam and (HOCH2CH2CH2)2( 4-CF3 PhCH2)2Cyclam, as well as their CuII and FeIII complexes, were synthesized and characterized and their stability in cellular media was assessed. The cytotoxic… Click to show full abstract

New cyclam derivatives (HOCH2CH2CH2)2(PhCH2)2Cyclam and (HOCH2CH2CH2)2( 4-CF3 PhCH2)2Cyclam, as well as their CuII and FeIII complexes, were synthesized and characterized and their stability in cellular media was assessed. The cytotoxic effect of all compounds was examined on human cervical cancer (HeLa) cells, revealing strong anticancer activity. After 24 h, only complexes with the (HOCH2CH2CH2)2( 4-CF3 PhCH2)2Cyclam ligand are cytotoxic, whereas after incubation for 72 h all compounds show significant antiproliferative effects. Notably, compounds containing 4-CF3 PhCH2 pendant arms on the cyclam ring revealed the most activity, with cytotoxicity values up to 12 times higher than those of cisplatin. All metal complexes seem to induce cell death through the formation of reactive oxygen species.

Keywords: cyclams copper; new cyclams; cf3 phch2; copper iron; anticancer; phch2 2cyclam

Journal Title: ChemMedChem
Year Published: 2019

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