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Cyclic (Alkyl)(Amino)Carbene (CAAC) Gold(I) Complexes as Chemotherapeutic Agents
Author(s) -
Proetto Maria T.,
Alexander Kelsey,
Melaimi Mohand,
Bertrand Guy,
Gianneschi Nathan C.
Publication year - 2021
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.202004317
Subject(s) - auranofin , hela , chemistry , carbene , combinatorial chemistry , gold compounds , rational design , ligand (biochemistry) , alkyl , ht1080 , stereochemistry , biophysics , cell , biochemistry , nanotechnology , biology , materials science , organic chemistry , receptor , rheumatoid arthritis , immunology , catalysis
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.