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Time-Dependent Cytotoxic Properties of Terpyridine-Based Copper Complexes.

Authors :: Grau J
Caubet A
Roubeau O
Montpeyó D
Lorenzo J
Gamez P
Source :: Chembiochem : a European journal of chemical biology [Chembiochem] 2020 Aug 17; Vol. 21 (16), pp. 2348-2355. Date of Electronic Publication: 2020 Apr 29.
Publication Year :: 2020
Abstract: Five copper complexes supported by terpyridine ligands were prepared and characterized, viz. [Cu <subscript>3</subscript> Cl <subscript>4</subscript> (naphtpy) <subscript>2</subscript> ][CuCl <subscript>2</subscript> ] (1), [Cu <subscript>2</subscript> Cl <subscript>2</subscript> (naphtpy) <subscript>2</subscript> ](ClO <subscript>4</subscript> ) <subscript>2</subscript> (2), [CuCl <subscript>2</subscript> (naphtpy)] <subscript>2</subscript> (MeOH) <subscript>3</subscript> (H <subscript>2</subscript> O) (3), [CuCl <subscript>2</subscript> (Cltpy)] (4) and [Cu(Cltpy) <subscript>2</subscript> ](ClO <subscript>4</subscript> ) <subscript>2</subscript> (5); (where naphtpy stands for 4'-((naphthalen-2-yl)methoxy)-2,2':6',2''-terpyridine and Cltpy for 4'-chloro-2,2':6',2''-terpyridine). Their ability to interact with DNA was investigated, and their cytotoxic behaviour was examined with three cells lines, namely human ovarian carcinoma cells (A2780), their derived cisplatin-resistant line (A2780cis), and human cervix adenocarcinoma cells (HeLa). All compounds show good cytotoxic properties (especially after 72 h of incubation). Remarkably, two compounds, 4 and 5, are still almost inactive after 24 h (particularly 4), but are highly active after 72 h, with IC <subscript>50</subscript> values in the low-micromolar to sub-micromolar range. Compounds 1 and 2 induce necrosis, whereas late apoptosis is observed with 3-5, 4 exhibiting a behaviour close to that of cisplatin.<br /> (© 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)