Abstract
Breast cancers (BCs) may present dramatic diagnoses, both for ineffective therapies and for the limited outcomes in terms of lifespan. For these types of tumors, the search for new drugs is a primary necessity. It is widely recognized that gold compounds are highly active and extremely potent as anticancer agents against many cancer cell lines. The presence of the metal plays an essential role in the activation of the cytotoxicity of these coordination compounds, whose activity, if restricted to the ligands alone, would be non-existent. On the other hand, gold exhibits a complex biochemistry, substantially variable depending on the chemical environments around the central metal. In this review, the scientific findings of the last 6–7 years on two classes of gold(I) compounds, containing phosphane or carbene ligands, are reviewed. In addition to this class of Au(I) compounds, the recent developments in the application of Auranofin in regards to BCs are reported. Auranofin is a triethylphosphine-thiosugar compound that, being a drug approved by the FDA—therefore extensively studied—is an interesting lead gold compound and a good comparison to understand the activities of structurally related Au(I) compounds.
Highlights
Some recent results in terms of IC50 are reported in Table 1 and, even though the values refer to different times of cell treatment, most of the phosphane gold(I) compounds resulted extremely active in regards to MCF7 or MDA-MB-231 cells, to cisplatin and Auranofin
We take into account the last works on two main categories of gold compounds, those containing phosphane groups and those containing carbene groups
thioredoxin reductase (TrxR) resulted to be the most strongly recognized and the most widely studied target, studies on residual activity on cancer cells highlighted other protein targets, characterized by the presence of cysteine residues in the catalytic site. It emerged a strong and diverse impact of the ligands bound to the Au center in tuning the binding affinity of the gold complexes towards molecular targets, resulting in a more complex mechanism of action than selective auration of the thiols or seleno-thiol protein groups
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Breast cancer is one of the most common forms of tumors for women and some subtypes of breast cancers are still without efficacious therapy. The search for new drugs with improved and wider efficacy is a current challenge. The present review focuses on the most relevant results reported in the scientific literature published over the last. 6–7 years about the in vitro and/or in vivo treatment of breast cancers by two classes of gold(I)-based drugs, phosphane and N-Heterocyclic Carbene (NHC) compounds, and on the main mechanism of actions thereby disclosed. The results are discussed comparatively to the classic metal-based drug, cisplatin, and to Auranofin
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