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The 20th Anniversary of Pharmaceuticals—Metal-Based Drugs for Cancer Treatment,...
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The 20th Anniversary of Pharmaceuticals—Metal-Based Drugs for Cancer Treatment, Antibacterial and Antiviral Applications

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (25 June 2024) | Viewed by 3120

Special Issue Editors

Dr. Alessandro Pratesi

E-Mail Website
Guest Editor
Department of Chemistry and Industrial Chemistry, University of Pisa, Via Giuseppe Moruzzi, 13, 56124 Pisa, Italy
Interests: inorganic chemistry; medicinal chemistry; bioinorganic chemistry; mass spectrometry; metal-based drugs; gold-based compounds, platinum-based compounds; drug targeting and delivery strategies; DNA and protein interactions; anticancer therapies; drug repurposing
Special Issues, Collections and Topics in MDPI journals
Dr. Damiano Cirri

E-Mail Website
Guest Editor
Department of Chemistry and Industrial Chemistry, University of Pisa, Via Giuseppe Moruzzi, 13, 56124 Pisa, Italy
Interests: bioinorganic chemistry; inorganic chemistry; NMR; metal-based drugs; chemotherapeutic agents
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Since the discovery of cisplatin in 1965 by Barnett Rosenberg, metal-based drugs have gained growing interest due to their great potential not only for the treatment of cancer, but also as effective bacterial and viral agents. The development of metal-based drugs with enhanced therapeutic properties has become a very active area of research. Metal-based drugs possess unique characteristics, such as chemical and structural diversity, high selectivity, and reactivity, which makes them promising for developing more effective treatments against a variety of diseases. They have been used to target cancer cells, bacteria, and viruses, either alone or in combination with other therapies. We invite authors to submit original research and review articles on the latest developments in metal-based compounds of medicinal interest. Topics of interest include, but are not limited to:     

  • The design, synthesis, and characterization of novel metal-based drugs;
  • The molecular mechanisms of action and resistance of metal-based drugs;   
  • Preclinical and clinical studies of metal-based compounds;      
  • Combinatorial approaches involving metallodrugs and other therapeutics;
  • Imaging and diagnostic applications of metal-based complexes. 

All submitted papers will undergo rigorous peer review by international experts in the field. The collection of accepted manuscripts will be published as a Special Issue in Pharmaceuticals, the 20th Anniversary series.

Dr. Alessandro Pratesi
Dr. Damiano Cirri
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • metal-based drugs
  • anticancer compounds
  • antivirals
  • antibiotics
  • chemotherapy
  • drug targeting
  • delivery strategies
  • drug repurposing
  • medicinal chemistry
  • bioinorganic chemistry

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Further information on MDPI's Special Issue polices can be found here.

Published Papers (2 papers)

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19 pages, 2863 KiB  
Article
Anticancer Activity of Imidazolyl Gold(I/III) Compounds in Non-Small Cell Lung Cancer Cell Lines
by Rossana Galassi, Nicola Sargentoni, Sofia Renzi, Lorenzo Luciani, Caterina Bartolacci, Prasad Pattabhi, Cristina Andreani and Stefania Pucciarelli
Pharmaceuticals 2024, 17(9), 1133; https://doi.org/10.3390/ph17091133 - 28 Aug 2024
Viewed by 863
Abstract
Lung cancer is a leading cause of cancer-related death worldwide that needs updated therapies to contrast both the serious side effects and the occurrence of drug resistance. A panel of non-small cell lung cancer (NSCLC) cells were herein employed as cancer models. Eight [...] Read more.
Lung cancer is a leading cause of cancer-related death worldwide that needs updated therapies to contrast both the serious side effects and the occurrence of drug resistance. A panel of non-small cell lung cancer (NSCLC) cells were herein employed as cancer models. Eight structurally related gold(I) and gold(III) complexes with NHC and halides or triphenylphosphane ligands were investigated as lung cancer cell growth inhibitors. As expected, gold compounds with PPh3 were found to be more cytotoxic than homoleptic [(NHC)2-Au(I)]X or heteroleptic NHC-Au(I)X or NHC-Au(III)X3 complexes. Mixed ligand gold(I) compounds exhibiting the linear NHC-AuPPh3 (compound 7) or the trigonal NHC-Au(Cl)PPh3 (compound 8) arrangements at the central metal were found to be the best lung cancer cytotoxic compounds. Analysis of the TrxR residual activity of the treated cells revealed that these compounds efficiently inhibit the most accredited molecular target for gold compounds, the TrxR, with compound 8 reaching more than 80% activity reduction in lung cells. Some of the current cancer lung therapy protocols consist of specific lung cancer cell cytotoxic agents combined with antifolate drugs; interestingly, the herein gold compounds are both TrxR and antifolate inhibitors. The human DHFR was inhibited with IC50 ranging between 10–21 µM, depending on substrate concentrations, proceeding by a likely allosteric mechanism only for compound 8. Full article
(This article belongs to the Special Issue The 20th Anniversary of Pharmaceuticals—Metal-Based Drugs for Cancer Treatment, Antibacterial and Antiviral Applications)
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16 pages, 2632 KiB  
Article
A Ru(II)-Strained Complex with 2,9-Diphenyl-1,10-phenanthroline Ligand Induces Selective Photoactivatable Chemotherapeutic Activity on Human Alveolar Carcinoma Cells via Apoptosis
by Najwa Mansour, Stephanie Mehanna, Kikki Bodman-Smith, Costantine F. Daher and Rony S. Khnayzer
Pharmaceuticals 2024, 17(1), 50; https://doi.org/10.3390/ph17010050 - 28 Dec 2023
Viewed by 1264
Abstract
[Ru(bipy)2(dpphen)]Cl2 (where bipy = 2,2′-bipyridine and dpphen = 2,9-diphenyl-1,10-phenanthroline) (complex 1) is a sterically strained compound that exhibits promising in vitro photocytotoxicity on an array of cell lines. Since lung adenocarcinoma cancer remains the most common lung cancer and [...] Read more.
[Ru(bipy)2(dpphen)]Cl2 (where bipy = 2,2′-bipyridine and dpphen = 2,9-diphenyl-1,10-phenanthroline) (complex 1) is a sterically strained compound that exhibits promising in vitro photocytotoxicity on an array of cell lines. Since lung adenocarcinoma cancer remains the most common lung cancer and the leading cause of cancer deaths, the current study aims to evaluate the plausible effect and uptake of complex 1 on human alveolar carcinoma cells (A549) and mesenchymal stem cells (MSC), and assess its cytotoxicity in vitro while considering its effect on cell morphology, membrane integrity and DNA damage. MSC and A549 cells showed similar rates of complex 1 uptake with a plateau at 12 h. Upon photoactivation, complex 1 exhibited selective, potent anticancer activity against A549 cells with phototoxicity index (PI) values of 16, 25 and 39 at 24, 48 and 72 h, respectively. This effect was accompanied by a significant increase in A549-cell rounding and detachment, loss of membrane integrity and DNA damage. Flow cytometry experiments confirmed that A549 cells undergo apoptosis when treated with complex 1 followed by photoactivation. In conclusion, this present study suggests that complex 1 might be a promising candidate for photochemotherapy with photoproducts that possess selective anticancer effects in vitro. These results are encouraging to probe the potential activity of this complex in vivo. Full article
(This article belongs to the Special Issue The 20th Anniversary of Pharmaceuticals—Metal-Based Drugs for Cancer Treatment, Antibacterial and Antiviral Applications)
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