Artificial chemical nuclease and cytotoxic activity of a mononuclear copper(I) complex and a related binuclear double‐stranded helicate

LEVÍN, PEDRO; BALSA, LUCÍA M.; SILVA, CARLOS P.; HERZOG, AUSTIN E.; VEGA, ANDRÉS; PAVEZ, JORGE; LEÓN, IGNACIO E.; LEMUS, LUIS

EUROPEAN JOURNAL OF INORGANIC CHEMISTRY

WILEY-V C H VERLAG GMBH

Año: 2021

1434-1948

Copper complexes are promissory candidates for anticancer drugs, because of theirredox properties and the ability to generate ROS in the cellular media. Most of thereported complexes with anticancer properties are based on Cu(II), which must bereduced to Cu(I) to exert the therapeutic action. Here, we report on the synthesis andcharacterization of two novel copper(I) complexes, a mononuclear complex[Cu(L1)2](ClO4) (1) and a binuclear helicate [Cu2(L2)2](ClO4)2 (2) (L1 = 2-ethoxy-1,10-phenanthroline, L2 = 1,2-bis((1,10-phenanthrolin-2-yl)oxy)ethane), which weredesigned to be structurally comparable, in order to evaluate the effect of nuclearity onthe artificial nuclease activity. The activity of helicate (2) was higher than that of themonometallic (1), and the DNA cleavage mechanism is through the generation ofhydroxyl radical in a Fenton-like reaction, where Cu(I) is oxidized by O2 as startingpoint. Also, helicate (2) showed a higher cytotoxic effect against different cancer cellslines, while both complexes are more active than cisplatin.