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Open AccessArticle

Is the Way to Fight Cancer Paved with Gold? Metal-Based Carbene Complexes with Multiple and Fascinating Biological Features

1
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, Italy
2
Biopolymers and Proteomics IRCCS, Ospedale Policlinico San Martino–IST, Largo R. Benzi 10, 16132 Genova, Italy
3
Department of Biology and Chemistry, University of Salerno, Via Giovanni Paolo II, 132, 84084 Fisciano, Italy
4
Department of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, Italy
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceuticals 2020, 13(5), 91; https://doi.org/10.3390/ph13050091
Received: 31 March 2020 / Revised: 28 April 2020 / Accepted: 8 May 2020 / Published: 11 May 2020
(This article belongs to the Section Medicinal Chemistry)
Herein, we report the synthesis and the multiple anti-tumor properties of new gold and silver carbene complexes. The chemical modifications, grounded on our previous studies, led us to identify a good lead complex, gold-based, whose biological features are very exciting and promising in the anti-cancer research and could be further developed. Indeed, the bis-[4,5-dichloro-(N-methyl-N’(2-hydroxy-2-phenyl)ethyl-imidazole-2-ylidene)gold(I)]+[dichloro-gold] (AuL7) complex possesses the ability to interfere with at least three important and different intracellular targets, namely the human topoisomerases I and II and tubulin, which are able to modulate metabolic processes not directly correlated each other. We proved that the modifications of the ligands structure in AuL7, with respect to another already published complex, i.e., bis-[4,5-dichloro-(N-methyl-N’(cyclopentane-2ol)-imidazole-2-ylidine)gold(I)]+[dichloro-gold] (AuL4), produce a different behavior toward tubulin-polymerization process, since AuL7 is a tubulin-polymerization inhibitor and AuL4 a stabilizer, with the final same result of hampering the tumor growth. Taken together, our outcomes designate AuL7 as a promising compound for the development of multi-targeted anti-cancer therapies. View Full-Text
Keywords: human topoisomerases I and II; tubulin; women cancers; docking studies; carbene complexes human topoisomerases I and II; tubulin; women cancers; docking studies; carbene complexes
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Iacopetta, D.; Rosano, C.; Sirignano, M.; Mariconda, A.; Ceramella, J.; Ponassi, M.; Saturnino, C.; Sinicropi, M.S.; Longo, P. Is the Way to Fight Cancer Paved with Gold? Metal-Based Carbene Complexes with Multiple and Fascinating Biological Features. Pharmaceuticals 2020, 13, 91.

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