Metallodrugs in Cancer Therapy: The Newest Candidates in the Field, 2nd Edition

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: 31 July 2024 | Viewed by 2002

Special Issue Editors


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Centro de Ciências Moleculares e Materiais, Departamento de Química e Bioquímica Faculdade de Ciências da Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal
Interests: metallodrugs; anti-cancer coordination compounds; biospeciation; therapeutic ruthenium/iron/copper compounds
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Centro de Química Estrutural, Institute of Molecular Sciences and Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal
Interests: anticancer drugs; cancer multidrug resistance; polymer–metal conjugates; drug delivery
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Centro de Química Estrutural, Institute of Molecular Sciences, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisboa, Portugal
Interests: anticancer drugs; drug delivery; metallodrugs; anti-cancer coordination compounds

Special Issue Information

Dear Colleagues,

Metal ions play key roles in a myriad of biological processes known to be essential to life. Living organisms have developed mechanisms to maintain cellular levels of metal ions, which are tightly regulated; excess or deficiency in these ions result in disease, including cancer disorders. The use of metals and their compounds as medicines has been known since ancient times, even though insight into their modes of action was merely empiric, and the distinction between a therapeutic or toxic dose was a major challenge. Metal compounds were long regarded with suspicion and undefined as humans’ ‘friends’ or ‘foes’; this was true until Rosenberg’s breakthrough on the properties of cisplatin more than sixty years ago, which consolidated the interest in metal compounds as useful potential therapeutics. Since then, three platinum complexes (cisplatin, oxaliplatin and carboplatin) have been approved for clinical use worldwide, and still stand out as the most often prescribed chemotherapeutics (applied in essentially every second therapeutic routine), being listed as ‘essential medicines’ by the World Health Organization despite the toxicity inherent to their use and multidrug resistance.

These benefits (remarkably high efficiency) and drawbacks (toxicity and resistance) ignited the interest in metallodrugs for chemotherapy. Today, this is a highly dynamic field of research that has spread to other metal-containing complexes as novel potential anticancer drugs. 

This Special Issue is intended to collect recent research/discoveries in the field of cancer prospective metallopharmaceuticals. This is an area in constant evolution, and we welcome submissions (research papers/focused reviews) on subjects including, but not limited to:

  • Synthetic methods/characterization and biological activity of novel metal-based compounds;
  • Structure–activity studies;
  • Drug delivery for metal-based compounds;
  • Metal complexes overcoming MDR (metallodrug resistance to treatment);
  • Mode of action, uptake, cell targets and (cyto)toxicity;
  • Metal complexes as theranostics;
  • Biospeciation of metal ions and anti-cancer metal-based compounds.

Dr. Ana Isabel Tomaz
Dr. Andreia Marques Valente
Dr. Leonor Côrte-Real
Guest Editors

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Published Papers (1 paper)

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Research

20 pages, 11922 KiB  
Article
Melatonin Derivative-Conjugated Formulations of Pd(II) and Pt(II) Thiazoline Complexes on Mesoporous Silica to Enhance Cytotoxicity and Apoptosis against HeLa Cells
by Samuel Estirado, Diana Díaz-García, Elena Fernández-Delgado, Emilio Viñuelas-Zahínos, Santiago Gómez-Ruiz, Sanjiv Prashar, Ana B. Rodríguez, Francisco Luna-Giles, José A. Pariente and Javier Espino
Pharmaceutics 2024, 16(1), 92; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics16010092 - 10 Jan 2024
Viewed by 1660
Abstract
The search for alternatives to cisplatin has led to the development of new metal complexes where thiazoline derivatives based on platinum(II) and palladium(II) stand out. In this sense, the Pt(II) and Pd(II) complexes coordinated with the thiazoline derivative ligand 2-(3,4-dichlorophenyl)imino-N-(2-thiazolin-2-yl)thiazolidine (TdTn), with formula [...] Read more.
The search for alternatives to cisplatin has led to the development of new metal complexes where thiazoline derivatives based on platinum(II) and palladium(II) stand out. In this sense, the Pt(II) and Pd(II) complexes coordinated with the thiazoline derivative ligand 2-(3,4-dichlorophenyl)imino-N-(2-thiazolin-2-yl)thiazolidine (TdTn), with formula [PtCl2(TdTn)] and [PdCl2(TdTn)], have previously shown good results against several cancer lines; however, in this work, we have managed to improve their activity by supporting them on mesoporous silica nanoparticles (MSN). The incorporation of metal compounds with a melatonin derivative (5-methoxytryptamine, 5MT), which is a well-known antioxidant and apoptosis inducer in different types of cancer, has been able to increase the cytotoxic activity of both MSN-supported and isolated complexes with only a very low amount (0.35% w/w) of this antioxidant. The covalently functionalized systems that have been synthesized are able to increase selectivity as well as accumulation in HeLa cells. The final materials containing the metal complexes and 5MT (MSN-5MT-PtTdTn and MSN-5MT-PdTdTn) required up to nine times less metal to achieve the same cytotoxic activity than their corresponding non-formulated counterparts did, thus reducing the potential side effects caused by the use of the free metal complexes. Full article
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