Issue 33, 2023

Fine-tuning the cytotoxicity of ruthenium(ii) arene compounds to enhance selectivity against breast cancers

Abstract

Ruthenium-based complexes have been suggested as promising anticancer drugs exhibiting reduced general toxicity compared to platinum-based drugs. In particular, Ru(η6-arene)(PTA)Cl2 (PTA = 1,3,5-triaza-7-phosphaadamantane), or RAPTA, complexes have demonstrated efficacy against breast cancer by suppressing metastasis, tumorigenicity, and inhibiting the replication of the human tumor suppressor gene BRCA1. However, RAPTA compounds have limited cytotoxicity, and therefore comparatively high doses are required. This study explores the activity of a series of RAPTA-like ruthenium(II) arene compounds against MCF-7 and MDA-MB-231 breast cancer cell lines and [Ru(η6-toluene)(PPh3)2Cl]+ was identified as a promising candidate. Notably, [Ru(η6-toluene)(PPh3)2Cl]Cl was found to be remarkably stable and highly cytotoxic, and selective to breast cancer cells. The minor groove of DNA was identified as a relevant target.

Graphical abstract: Fine-tuning the cytotoxicity of ruthenium(ii) arene compounds to enhance selectivity against breast cancers

Supplementary files

Article information

Article type
Paper
Submitted
29 Jun 2023
Accepted
28 Jul 2023
First published
28 Jul 2023
This article is Open Access
Creative Commons BY license

Dalton Trans., 2023,52, 11679-11690

Fine-tuning the cytotoxicity of ruthenium(II) arene compounds to enhance selectivity against breast cancers

S. A. P. Pereira, J. Romano-deGea, A. I. Barbosa, S. A. Costa Lima, P. J. Dyson and M. L. M. F. S. Saraiva, Dalton Trans., 2023, 52, 11679 DOI: 10.1039/D3DT02037A

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