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New Cyclams and Their Copper(II) and Iron(III) Complexes: Synthesis and Potential Application as Anticancer Agents
Author(s) -
Pilon Adhan,
Lorenzo Julia,
RodriguezCalado Sergi,
Adão Pedro,
Martins Ana M.,
Valente Andreia,
Alves Luis G.
Publication year - 2019
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201800702
Subject(s) - cyclam , hela , cisplatin , cytotoxicity , cytotoxic t cell , chemistry , reactive oxygen species , ligand (biochemistry) , metal , stereochemistry , biochemistry , biology , in vitro , receptor , organic chemistry , chemotherapy , genetics
New cyclam derivatives (HOCH 2 CH 2 CH 2 ) 2 (PhCH 2 ) 2 Cyclam and (HOCH 2 CH 2 CH 2 ) 2 (4 - CF3PhCH 2 ) 2 Cyclam, as well as their Cu II and Fe III 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 (HOCH 2 CH 2 CH 2 ) 2 (4 - CF3PhCH 2 ) 2 Cyclam ligand are cytotoxic, whereas after incubation for 72 h all compounds show significant antiproliferative effects. Notably, compounds containing4 - CF3PhCH 2 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.