Current Advances, Applications and Future Development of Transition Metal Complexes, 2nd Edition

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

Deadline for manuscript submissions: 25 January 2026 | Viewed by 149

Special Issue Editor


E-Mail Website
Guest Editor
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
Special Issues, Collections and Topics in MDPI journals

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 have 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 generation of drugs that could overcome the usual disadvantages of current drug therapies, such as 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 developed in order to shed light on the biological, pharmacological, and molecular mechanisms of metallodrugs in complex biological systems, since these play a key role in drug development and the improvement of patient 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

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 250 words) can be sent to the Editorial Office for assessment.

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

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

Benefits of Publishing in a Special Issue

  • Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
  • Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
  • Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
  • External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
  • Reprint: MDPI Books provides the opportunity to republish successful Special Issues in book format, both online and in print.

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

Published Papers (1 paper)

Order results
Result details
Select all
Export citation of selected articles as:

Research

42 pages, 6181 KB  
Article
1-Azinyl-1′-Alkenylferrocenes with Anticholinesterase, Antioxidant, and Antiaggregating Activities as Multifunctional Agents for Potential Treatment of Alzheimer’s Disease
by Galina F. Makhaeva, Irina A. Utepova, Elena V. Rudakova, Nadezhda V. Kovaleva, Natalia P. Boltneva, Elena Yu. Zyryanova, Alexandra A. Musikhina, Vladimir F. Lazarev, Snezhana A. Vladimirova, Irina V. Guzhova, Ilya N. Ganebnykh, Tatiana Y. Astakhova, Elena N. Timokhina, Oleg N. Chupakhin, Valery N. Charushin and Rudy J. Richardson
Pharmaceuticals 2025, 18(12), 1862; https://doi.org/10.3390/ph18121862 - 5 Dec 2025
Abstract
Background/Objectives: This study focused on synthesizing novel alkenyl derivatives of azinylferrocenes and evaluating their potential as Alzheimer’s disease (AD) therapeutics. Methods: 1-Azinyl-1′-acetylferrocenes were obtained by regioselective acetylation of azinylferrocenes, followed by the Wittig reaction or reduction of 1-azinyl-1′-acetylferrocenes and subsequent dehydration [...] Read more.
Background/Objectives: This study focused on synthesizing novel alkenyl derivatives of azinylferrocenes and evaluating their potential as Alzheimer’s disease (AD) therapeutics. Methods: 1-Azinyl-1′-acetylferrocenes were obtained by regioselective acetylation of azinylferrocenes, followed by the Wittig reaction or reduction of 1-azinyl-1′-acetylferrocenes and subsequent dehydration of the resulting alcohols. The synthesized compounds underwent the following biological activity testing relevant to AD: inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and off-target carboxylesterase (CES); antioxidant capacity (ABTS and FRAP assays); inhibition of Aβ42 self-aggregation (thioflavin method); blocking AChE-induced β-amyloid aggregation (propidium displacement); and cytotoxicity in SH-SY5Y and MSC-Neu cells (MTT assay). Results: Quinoline and bipyridine derivatives demonstrated effective cholinesterase inhibition, especially quinoline 7b (AChE IC50 3.32 μM; BChE IC50 3.68 μM), while acridine derivatives were poor inhibitors. Quantum chemical (QC) calculations predicted that acridine derivatives were especially prone to form stable dimers. Molecular docking into protein targets generated by an AlphaFold3 reproduction code showed that these dimers were too bulky to access enzyme active sites, yet they could bind to protein surfaces to inhibit Aβ42 self-aggregation and displace propidium from the AChE peripheral anionic site. All compounds showed high antioxidant activity in ABTS and FRAP assays, with quinoline derivatives being 2–4 times more potent than Trolox. QC calculations supported these findings. Quinoline and bipyridine derivatives also exhibited low cytotoxicity and scant CES inhibition. Conclusions: Overall, the synthesized ferrocenes, particularly the quinoline and bipyridine derivatives, appear promising for further research as multifunctional therapeutic agents targeting AD due to their anticholinesterase, antiaggregating, and antioxidant activities combined with low toxicity. Full article
Show Figures

Graphical abstract

Back to TopTop