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

Chembiochem

nanoBIC, Department of Inorganic and Organic Chemistry Inorganic Chemistry Section, University of Barcelona, Martí i Franquès 1-11, 08028, Barcelona, Spain.

Published: August 2020

AI Article Synopsis

  • Five copper complexes with different terpyridine ligands were synthesized and analyzed for their properties and effectiveness against cancer cells.
  • Their interactions with DNA were studied, and they were tested on three types of cancer cell lines: A2780 (human ovarian carcinoma), A2780cis (cisplatin-resistant), and HeLa (human cervix adenocarcinoma).
  • All complexes showed notable cytotoxicity, particularly after 72 hours, with two compounds (4 and 5) becoming significantly more effective over time, while compounds 1 and 2 caused necrosis, and compounds 3-5 led to late apoptosis similar to cisplatin's effects.

Article Abstract

Five copper complexes supported by terpyridine ligands were prepared and characterized, viz. [Cu Cl (naphtpy) ][CuCl ] (1), [Cu Cl (naphtpy) ](ClO ) (2), [CuCl (naphtpy)] (MeOH) (H O) (3), [CuCl (Cltpy)] (4) and [Cu(Cltpy) ](ClO ) (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 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.

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http://dx.doi.org/10.1002/cbic.202000154DOI Listing

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