Current Advances, Applications and Future Development of Transition Metal Complexes

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

Deadline for manuscript submissions: 30 May 2025 | Viewed by 5011

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Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via Pietro Bucci, 87036 Arcavacata di Rende, Italy
Interests: food; medicinal chemistry; bioactive products; nutraceuticals; phytochemicals; natural products extraction and isolation; antioxidants; anti-inflammatory; antimicrobials enzyme inhibition; cancer; cell biology
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Special Issue Information

Dear Colleagues,

Metal ions play fundamental roles in several biological processes, from electron transfer to catalysis and structural roles, and are frequently associated with active sites of proteins and enzymes. Thus, the medicinal applications of metals and their complexes are becoming clinically and commercially intriguing. Nowadays, the heterocyclic ligand complexes, especially with transition metals, have attracted the attention of several researchers because of their wide range of biological activities, namely antibacterial, antifungal, antitumor, antiviral, etc. Aside from their pharmaceutical role, transition metal complexes have been successfully employed as diagnostic agents. Moreover, their unique characteristics, including redox activity, variable coordination modes and reactivity towards organic substrates, made them very attractive probes in medicinal chemistry. The unique properties of transition metal complexes brought fascinating therapeutic applications to the development of metal-based drugs. The study of transition metal complexes, together with targeting and activation strategies, is fundamental for the synthesis of the next generations of drugs that could overcome the usual disadvantages of the current drug therapies, as the dramatic side effects and resistance phenomena onset, with the hope of widening the activity spectrum and tailoring their use ad personam. The field of medicinal inorganic chemistry and interdisciplinary research on metallodrugs needs to be further evolved to shed light on the biological, pharmacological and molecular mechanisms of metallodrugs in the complex biological systems, playing a key role in drug development and improving the patient's quality of life.

This Special Issue welcomes innovative research and review papers dealing with several aspects of the design, synthesis, characterization and biological evaluation of transition metal complexes for the development of novel therapeutic tools in medicinal chemistry.

Dr. Domenico Iacopetta
Guest Editor

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Keywords

  • transition metal complexes
  • synthesis
  • catalysis
  • ligands
  • biological activity
  • applications
  • enzyme inhibition

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Published Papers (2 papers)

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Research

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19 pages, 3342 KiB  
Article
Designing and Exploration of the Biological Potentials of Novel Centrosymmetric Heteroleptic Copper(II) Carboxylates
by Viola, Niaz Muhammad, Awal Noor, Muhammad Sirajuddin, Maciej Kubicki, Shahnaz Rahim, Abdus Samad, Shaukat Shujah, Abdul Wadood and Saqib Ali
Pharmaceuticals 2023, 16(10), 1462; https://doi.org/10.3390/ph16101462 - 14 Oct 2023
Cited by 3 | Viewed by 1285
Abstract
Copper(II) complexes with a general formula [Cu2(3,4-F2C6H3CH2COO)4(L)2], where L = 2-methylpyridine (1) and 3-methylpyridine (2), are reported here. The FTIR spectra of the complexes confirmed [...] Read more.
Copper(II) complexes with a general formula [Cu2(3,4-F2C6H3CH2COO)4(L)2], where L = 2-methylpyridine (1) and 3-methylpyridine (2), are reported here. The FTIR spectra of the complexes confirmed the bridging bidentate coordination mode of the carboxylate ligand. The low (475 and 449 cm−1) and strong (727 & 725 cm−1) intensity bands in the FTIR spectra, due to Cu-N stretches and pyridyl ring vibrations, confirmed coordination of the 2-/3-methyl pyridine co-ligands in complexes 1 and 2, respectively. A binuclear paddlewheel structural arrangement with a square pyramidal geometry was confirmed for copper atoms in the complexes via single-crystal X-ray analysis. The DPPH, OH radical, and α-amylase enzyme inhibition assays showed higher activities for the complexes than for the free ligand acid. The binding constant (Kb = 1.32 × 105 for 1 and 5.33 × 105 for 2) calculated via UV-VIS absorption measurements and docking scores (−6.59 for 1 and −7.43 for 2) calculated via molecular docking showed higher SS-DNA binding potential for 2 compared to 1. Viscosity measurement also reflected higher DNA binding ability for 2 than 1. Both complexes 1 and 2 (docking scores of −7.43 and −6.95, respectively) were found to be more active inhibitors than the free ligand acid (docking score of −5.5159) against the target α-amylase protein. This in silico study has shown that the herein reported compounds follow the rules of drug-likeness and exhibit good potential for bioavailability. Full article
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Review

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32 pages, 10134 KiB  
Review
Complexes of Ruthenium(II) as Promising Dual-Active Agents against Cancer and Viral Infections
by Assunta D’Amato, Annaluisa Mariconda, Domenico Iacopetta, Jessica Ceramella, Alessia Catalano, Maria Stefania Sinicropi and Pasquale Longo
Pharmaceuticals 2023, 16(12), 1729; https://doi.org/10.3390/ph16121729 - 15 Dec 2023
Cited by 9 | Viewed by 3004
Abstract
Poor responses to medical care and the failure of pharmacological treatment for many high-frequency diseases, such as cancer and viral infections, have been widely documented. In this context, numerous metal-based substances, including cisplatin, auranofin, various gold metallodrugs, and ruthenium complexes, are under study [...] Read more.
Poor responses to medical care and the failure of pharmacological treatment for many high-frequency diseases, such as cancer and viral infections, have been widely documented. In this context, numerous metal-based substances, including cisplatin, auranofin, various gold metallodrugs, and ruthenium complexes, are under study as possible anticancer and antiviral agents. The two Ru(III) and Ru(II) complexes, namely, BOLD-100 and RAPTA-C, are presently being studied in a clinical trial and preclinical studies evaluation, respectively, as anticancer agents. Interestingly, BOLD-100 has also recently demonstrated antiviral activity against SARS-CoV-2, which is the virus responsible for the COVID-19 pandemic. Over the last years, much effort has been dedicated to discovering new dual anticancer–antiviral agents. Ru-based complexes could be very suitable in this respect. Thus, this review focuses on the most recent studies regarding newly synthesized Ru(II) complexes for use as anticancer and/or antiviral agents. Full article
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Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

Title: Antitumoral activity of silver and gold(I) complexes having chiral NHC ligands.
Author: Longo
Highlights: Synthesis of NHC ligand with chiral substituents on nitrogen atoms. Silver and Gold Complexes with chiral NHC ligands Anticancer acitivity of chiral NHC silver and gold complexes in vitro

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