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Cyclic (Alkyl)(Amino)Carbene (CAAC) Gold(I) Complexes as Chemotherapeutic Agents.

Authors :
Proetto MT
Alexander K
Melaimi M
Bertrand G
Gianneschi NC
Source :
Chemistry (Weinheim an der Bergstrasse, Germany) [Chemistry] 2021 Feb 19; Vol. 27 (11), pp. 3772-3778. Date of Electronic Publication: 2021 Jan 19.
Publication Year :
2021

Abstract

Cyclic (Alkyl)(Amino)Carbenes (CAACs) have become forceful ligands for gold due to their ability to form very strong ligand-metal bonds. Inspired by the success of Auranofin and other gold complexes as antitumor agents, we have studied the cytotoxicity of bis- and mono-CAAC-gold complexes on different cancer cell lines: HeLa (cervical cancer), A549 (lung cancer), HT1080 (fibrosarcoma) and Caov-3 (ovarian cancer). Further investigations aimed at elucidating their mechanism of action are described. This includes quantification of affinities for TrxR, evaluation of their bioavailability and determination of associated cell death process. Moreover, Transmission Electron Microscopy (TEM) was used to study morphological changes upon exposure. Noticeably, a significant reduction in non-specific binding to serum proteins was observed with CAAC complexes when compared to Auranofin. These results confirm the potential of CAAC-gold complexes in biological environments, which may result in more specific drug-target interactions and decreased side effects.<br /> (© 2020 Wiley-VCH GmbH.)

Details

Language :
English
ISSN :
1521-3765
Volume :
27
Issue :
11
Database :
MEDLINE
Journal :
Chemistry (Weinheim an der Bergstrasse, Germany)
Publication Type :
Academic Journal
Accession number :
33090571
Full Text :
https://doi.org/10.1002/chem.202004317