Research

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15 pages, 3473 KiB

Open AccessArticle

Novel Biotinylated Cu(II)-Phenanthroline Complexes: 2D and 3D Cytotoxic Activity and Mechanistic Insight

by Stephen Barrett, Michele De Franco, Chiara Donati, Cristina Marzano, Valentina Gandin and Diego Montagner

Molecules 2023, 28(10), 4112; https://doi.org/10.3390/molecules28104112 - 16 May 2023

Cited by 1 | Viewed by 1298

Abstract

The interest in the use of copper as a metal scaffold for the development of novel chemotherapeutics has considerably grown in recent years. This is mainly due to the relatively lower toxicity of copper complexes with respect to platinum drugs (i.e., cisplatin), the [...] Read more.

The interest in the use of copper as a metal scaffold for the development of novel chemotherapeutics has considerably grown in recent years. This is mainly due to the relatively lower toxicity of copper complexes with respect to platinum drugs (i.e., cisplatin), the different mechanisms of action, and the cheaper cost. In the last decades, hundreds of copper-based complexes were developed and screened as anticancer agents, with the antesignanus of all compounds being copper bis-phenanthroline [Cu(phen)₂]²⁺ developed by D.S. Sigman in the late 1990s. In particular, copper(phen) derivatives have been shown high interest in their capacity to interact with DNA by nucleobase intercalation. Here, we report the synthesis and chemical characterization of four novel copper(II) complexes functionalised with phenanthroline derivatives containing biotin. Biotin, also known as Vitamin B7, is involved in a series of metabolic processes, and its receptors are often overexpressed in many tumour cells. A detailed biological analysis including cytotoxicity in 2D and 3D, cellular drug uptake, DNA interaction, and morphological studies are discussed. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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16 pages, 2111 KiB

Open AccessArticle

Investigating the Interaction of an Anticancer Nucleolipidic Ru(III) Complex with Human Serum Proteins: A Spectroscopic Study

by Claudia Riccardi, Antonella Campanella, Daniela Montesarchio, Pompea Del Vecchio, Rosario Oliva and Luigi Paduano

Molecules 2023, 28(6), 2800; https://doi.org/10.3390/molecules28062800 - 20 Mar 2023

Cited by 1 | Viewed by 1426

Abstract

Ruthenium(III) complexes are very promising candidates as metal-based anticancer drugs, and several studies have supported the likely role of human serum proteins in the transport and selective delivery of Ru(III)-based compounds to tumor cells. Herein, the anticancer nanosystem composed of an amphiphilic nucleolipid [...] Read more.

Ruthenium(III) complexes are very promising candidates as metal-based anticancer drugs, and several studies have supported the likely role of human serum proteins in the transport and selective delivery of Ru(III)-based compounds to tumor cells. Herein, the anticancer nanosystem composed of an amphiphilic nucleolipid incorporating a Ru(III) complex, which we named DoHuRu, embedded into the biocompatible cationic lipid DOTAP, was investigated as to its interaction with two human serum proteins thought to be involved in the mechanism of action of Ru(III)-based anticancer drugs, i.e., human serum albumin (HSA) and human transferrin (hTf). This nanosystem was studied in comparison with the simple Ru(III) complex named AziRu, a low molecular weight metal complex previously designed as an analogue of NAMI-A, decorated with the same ruthenium ligands as DoHuRu but devoid of the nucleolipid scaffold and not inserted in liposomal formulations. For this study, different spectroscopic techniques, i.e., Fluorescence Spectroscopy and Circular Dichroism (CD), were exploited, showing that DoHuRu/DOTAP liposomes can interact with both serum proteins without affecting their secondary structures. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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21 pages, 8464 KiB

Open AccessArticle

Synthesis and Antiparasitic Activity of New Trithiolato-Bridged Dinuclear Ruthenium(II)-arene-carbohydrate Conjugates

by Isabelle Holzer, Oksana Desiatkina, Nicoleta Anghel, Serena K. Johns, Ghalia Boubaker, Andrew Hemphill, Julien Furrer and Emilia Păunescu

Molecules 2023, 28(2), 902; https://doi.org/10.3390/molecules28020902 - 16 Jan 2023

Cited by 3 | Viewed by 1784

Abstract

Eight novel carbohydrate-tethered trithiolato dinuclear ruthenium(II)-arene complexes were synthesized using CuAAC ‘click’ (Cu(I)-catalyzed azide-alkyne cycloaddition) reactions, and there in vitro activity against transgenic T. gondii tachyzoites constitutively expressing β-galactosidase (T. gondii β-gal) and in non-infected human foreskin fibroblasts, HFF, was determined at [...] Read more.

Eight novel carbohydrate-tethered trithiolato dinuclear ruthenium(II)-arene complexes were synthesized using CuAAC ‘click’ (Cu(I)-catalyzed azide-alkyne cycloaddition) reactions, and there in vitro activity against transgenic T. gondii tachyzoites constitutively expressing β-galactosidase (T. gondii β-gal) and in non-infected human foreskin fibroblasts, HFF, was determined at 0.1 and 1 µM. When evaluated at 1 µM, seven diruthenium-carbohydrate conjugates strongly impaired parasite proliferation by >90%, while HFF viability was retained at 50% or more, and they were further subjected to the half-maximal inhibitory concentration (IC₅₀) measurement on T. gondii β-gal. Results revealed that the biological activity of the hybrids was influenced both by the nature of the carbohydrate (glucose vs. galactose) appended on ruthenium complex and the type/length of the linker between the two units. 23 and 26, two galactose-based diruthenium conjugates, exhibited low IC₅₀ values and reduced effect on HFF viability when applied at 2.5 µM (23: IC₅₀ = 0.032 µM/HFF viability 92% and 26: IC₅₀ = 0.153 µM/HFF viability 97%). Remarkably, compounds 23 and 26 performed significantly better than the corresponding carbohydrate non-modified diruthenium complexes, showing that this type of conjugates are a promising approach for obtaining new antiparasitic compounds with reduced toxicity. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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24 pages, 4660 KiB

Open AccessArticle

Green Extracellular Synthesis of Silver Nanoparticles by Pseudomonas alloputida, Their Growth and Biofilm-Formation Inhibitory Activities and Synergic Behavior with Three Classical Antibiotics

by Carlos Pernas-Pleite, Amparo M. Conejo-Martínez, Irma Marín and José P. Abad

Molecules 2022, 27(21), 7589; https://doi.org/10.3390/molecules27217589 - 05 Nov 2022

Cited by 4 | Viewed by 1863

Abstract

Bacterial resistance to antibiotics is on the rise and hinders the fight against bacterial infections, which are expected to cause millions of deaths by 2050. New antibiotics are difficult to find, so alternatives are needed. One could be metal-based drugs, such as silver [...] Read more.

Bacterial resistance to antibiotics is on the rise and hinders the fight against bacterial infections, which are expected to cause millions of deaths by 2050. New antibiotics are difficult to find, so alternatives are needed. One could be metal-based drugs, such as silver nanoparticles (AgNPs). In general, chemical methods for AgNPs’ production are potentially toxic, and the physical ones expensive, while green approaches are not. In this paper, we present the green synthesis of AgNPs using two Pseudomonas alloputida B003 UAM culture broths, sampled from their exponential and stationary growth phases. AgNPs were physicochemically characterized by transmission electron microscopy (TEM), total reflection X-ray fluorescence (TXRF), infrared spectroscopy (FTIR), dynamic light scattering (DLS), and X-ray diffraction (XRD), showing differential characteristics depending on the synthesis method used. Antibacterial activity was tested in three assays, and we compared the growth and biofilm-formation inhibition of six test bacteria: Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis. We also monitored nanoparticles’ synergic behavior through the growth inhibition of E. coli and S. aureus by three classical antibiotics: ampicillin, nalidixic acid, and streptomycin. The results indicate that very good AgNP activity was obtained with particularly low MICs for the three tested strains of P. aeruginosa. A good synergistic effect on streptomycin activity was observed for all the nanoparticles. For ampicillin, a synergic effect was detected only against S. aureus. ROS production was found to be related to the AgNPs’ antibacterial activity. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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15 pages, 29690 KiB

Open AccessArticle

Rubus Capped Zinc Oxide Nanoparticles Induce Apoptosis in MCF-7 Breast Cancer Cells

by Blassan P. George, Naresh K. Rajendran, Nicolette N. Houreld and Heidi Abrahamse

Molecules 2022, 27(20), 6862; https://doi.org/10.3390/molecules27206862 - 13 Oct 2022

Cited by 5 | Viewed by 1665

Abstract

Rubus fairholmianus (RF) has widely been used to treat various ailments, including pain, diabetes, and cancer. Zinc oxide nanoparticles (ZnO NPs) have drawn attention in modern healthcare applications. Hence, we designed this study to synthesize zinc oxide (ZnO) nanoparticles using R. fairholmianus root [...] Read more.

Rubus fairholmianus (RF) has widely been used to treat various ailments, including pain, diabetes, and cancer. Zinc oxide nanoparticles (ZnO NPs) have drawn attention in modern healthcare applications. Hence, we designed this study to synthesize zinc oxide (ZnO) nanoparticles using R. fairholmianus root extract to investigate its synergistic cytotoxic effect on MCF-7 cells and explore the possible cell death mechanism. ZnO NPs were synthesized via green synthesis using R. fairholmianus root extract, and the effect on MCF-7 cells was determined by looking at cellular morphology, proliferation, cytotoxicity, apoptosis, and reactive oxygen species (ROS). The results showed that cellular proliferation was reduced following treatment with R. fairholmianus capped zinc oxide nanoparticles (RFZnO NPs), while cytotoxicity and ROS were increased. There was also an increase in apoptosis as indicated by the significant increase in cytoplasmic cytochrome c and caspase 3/7 (markers of apoptosis), as well as increased levels of pro-apoptotic proteins (p53, Bax) and decreased levels of anti-apoptotic protein (Bcl-2). In conclusion, these results showed that RFZnO NPs induce apoptosis in breast cancer cells via a mitochondria-mediated caspase-dependent apoptotic pathway and suggest the use of acetone root extract of R. fairholmianus for the treatment of cancer-related ailments. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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11 pages, 3336 KiB

Open AccessArticle

Structural Characterization of Cis– and Trans–Pt(NH₃)₂Cl₂ Conjugations with Chitosan Nanoparticles

by Penparapa Chanphai, Gervais Bérubé and Heidar-Ali Tajmir-Riahi

Molecules 2022, 27(19), 6264; https://doi.org/10.3390/molecules27196264 - 23 Sep 2022

Cited by 1 | Viewed by 880

Abstract

The conjugation of chitosan 15 and 100 KD with anticancer drugs cis– and trans–Pt (NH₃)₂Cl₂ (abbreviated cis–Pt and trans–Pt) were studied at pH 5–6. Using multiple spectroscopic methods and thermodynamic analysis to characterize the nature of drug–chitosan interactions [...] Read more.

The conjugation of chitosan 15 and 100 KD with anticancer drugs cis– and trans–Pt (NH₃)₂Cl₂ (abbreviated cis–Pt and trans–Pt) were studied at pH 5–6. Using multiple spectroscopic methods and thermodynamic analysis to characterize the nature of drug–chitosan interactions and the potential application of chitosan nanoparticles in drug delivery. Analysis showed that both hydrophobic and hydrophilic contacts are involved in drug–polymer interactions, while chitosan size and charge play a major role in the stability of drug–polymer complexes. The overall binding constants are K_{ch–15–cis–Pt} = 1.44 (±0.6) × 10⁵ M⁻¹, K_{ch–100–cis–Pt} = 1.89 (±0.9) × 10⁵ M⁻¹ and K_{ch–15–trans–Pt} = 9.84 (±0.5) × 10⁴ M⁻¹, and K_{ch–100–trans–Pt} = 1.15 (±0.6) × 10⁵ M⁻¹. More stable complexes were formed with cis–Pt than with trans–Pt–chitosan adducts, while stronger binding was observed for chitosan 100 in comparison to chitosan 15 KD. This study indicates that polymer chitosan 100 is a stronger drug carrier than chitosan 15 KD in vitro. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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20 pages, 9238 KiB

Open AccessArticle

Multispectral and Molecular Docking Studies Reveal Potential Effectiveness of Antidepressant Fluoxetine by Forming π-Acceptor Complexes

by Ahmed Gaber, Walaa F. Alsanie, Majid Alhomrani, Abdulhakeem S. Alamri, Hussain Alyami, Sonam Shakya, Hamza Habeeballah, Heba A. Alkhatabi, Raed I. Felimban, Abdulwahab Alamri, Abdulhameed Abdullah Alhabeeb, Bassem M. Raafat and Moamen S. Refat

Molecules 2022, 27(18), 5883; https://doi.org/10.3390/molecules27185883 - 10 Sep 2022

Viewed by 1879

Abstract

Poor mood, lack of pleasure, reduced focus, remorse, unpleasant thoughts, and sleep difficulties are all symptoms of depression. The only approved treatment for children and adolescents with major depressive disorder (MDD) is fluoxetine hydrochloride (FXN), a serotonin selective reuptake inhibitor antidepressant. MDD is [...] Read more.

Poor mood, lack of pleasure, reduced focus, remorse, unpleasant thoughts, and sleep difficulties are all symptoms of depression. The only approved treatment for children and adolescents with major depressive disorder (MDD) is fluoxetine hydrochloride (FXN), a serotonin selective reuptake inhibitor antidepressant. MDD is the most common cause of disability worldwide. In the present research, picric acid (PA); dinitrobenzene; p-nitro benzoic acid; 2,6-dichloroquinone-4-chloroimide; 2,6-dibromoquinone-4-chloroimide; and 7,7′,8,8′-tetracyanoquinodimethane were used to make 1:1 FXN charge-transfer compounds in solid and liquid forms. The isolated complexes were then characterized by elemental analysis, conductivity, infrared, Raman, and ¹H-NMR spectra, thermogravimetric analysis, scanning electron microscopy, and X-ray powder diffraction. Additionally, a molecular docking investigation was conducted on the donor moiety using FXN alone and the resulting charge transfer complex [(FXN)(PA)] as an acceptor to examine the interactions against two protein receptors (serotonin or dopamine). Interestingly, the [(FXN)(PA)] complex binds to both serotonin and dopamine more effectively than the FXN drug alone. Furthermore, [(FXN)(PA)]–serotonin had a greater binding energy than [FXN]–serotonin. Theoretical data were also generated by density functional theory simulations, which aided the molecular geometry investigation and could be beneficial to researchers in the future. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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19 pages, 9751 KiB

Open AccessArticle

Spectroscopic and Molecular Docking Studies of Cu(II), Ni(II), Co(II), and Mn(II) Complexes with Anticonvulsant Therapeutic Agent Gabapentin

by Moamen S. Refat, Ahmed Gaber, Yusuf S. Althobaiti, Hussain Alyami, Walaa F. Alsanie, Sonam Shakya, Abdel Majid A. Adam, Mohamed I. Kobeasy and Kareem A. Asla

Molecules 2022, 27(13), 4311; https://doi.org/10.3390/molecules27134311 - 05 Jul 2022

Cited by 6 | Viewed by 1786

Abstract

New Cu(II), Ni(II), Co(II), and Mn(II) complexes of the gabapentin (Gpn) bidentate drug ligand were synthesized and studied using elemental analyses, melting temperatures, molar conductivity, UV–Vis, magnetic measurements, FTIR, and surface morphology (scanning (SEM) and transmission (TEM) electron microscopes).The gabapentin ligand was shown [...] Read more.

New Cu(II), Ni(II), Co(II), and Mn(II) complexes of the gabapentin (Gpn) bidentate drug ligand were synthesized and studied using elemental analyses, melting temperatures, molar conductivity, UV–Vis, magnetic measurements, FTIR, and surface morphology (scanning (SEM) and transmission (TEM) electron microscopes).The gabapentin ligand was shown to form monobasic metal:ligand (1:1) stoichiometry complexes with the metal ions Cu(II), Ni(II), Co(II), and Mn(II). Molar conductance measurements in dimethyl-sulfoxide solvent with a concentration of 10⁻³ M correlated to a non-electrolytic character for all of the produced complexes. A deformed octahedral environment was proposed for all metal complexes. Through the nitrogen atom of the –NH₂ group and the oxygen atom of the carboxylate group, the Gpn drug chelated as a bidentate ligand toward the Mn²⁺, Co²⁺, Ni²⁺, and Cu²⁺ metal ions. This coordination behavior was validated by spectroscopic, magnetic, and electronic spectra using the formulas of the [M(Gpn)(H₂O)₃(Cl)]·nH₂O complexes (where n = 2–6).Transmission electron microscopy was used to examine the nanostructure of the produced gabapentin complexes. Molecular docking was utilized to investigate the comparative interaction between the Gpn drug and its four metal [Cu(II), Ni(II), Co(II), and Mn(II)] complexes as ligands using serotonin (6BQH) and dopamine (6CM4) receptors. AutoDock Vina results were further refined through molecular dynamics simulation, and molecular processes for receptor–ligand interactions were also studied. The B3LYP level of theory and LanL2DZ basis set was used for DFT (density functional theory) studies. The optimized geometries, along with the MEP map and HOMO → LUMO of the metal complexes, were studied. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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22 pages, 2486 KiB

Open AccessArticle

Screening of Specific and Common Pathways in Breast Cancer Cell Lines MCF-7 and MDA-MB-231 Treated with Chlorophyllides Composites

by Keng-Shiang Huang, Yi-Ting Wang, Omkar Byadgi, Ting-Yu Huang, Mi-Hsueh Tai, Jei-Fu Shaw and Chih-Hui Yang

Molecules 2022, 27(12), 3950; https://doi.org/10.3390/molecules27123950 - 20 Jun 2022

Cited by 3 | Viewed by 2242

Abstract

Our previous findings have shown that the chlorophyllides composites have anticancer activities to breast cancer cell lines (MCF-7 and MDA-MB-231). In the present study, microarray gene expression profiling was utilized to investigate the chlorophyllides anticancer mechanism on the breast cancer cells lines. Results [...] Read more.

Our previous findings have shown that the chlorophyllides composites have anticancer activities to breast cancer cell lines (MCF-7 and MDA-MB-231). In the present study, microarray gene expression profiling was utilized to investigate the chlorophyllides anticancer mechanism on the breast cancer cells lines. Results showed that chlorophyllides composites induced upregulation of 43 and 56 differentially expressed genes (DEG) in MCF-7 and MDA-MB-231 cells, respectively. In both cell lines, chlorophyllides composites modulated the expression of annexin A4 (ANXA4), chemokine C-C motif receptor 1 (CCR1), stromal interaction molecule 2 (STIM2), ethanolamine kinase 1 (ETNK1) and member of RAS oncogene family (RAP2B). Further, the KEGG annotation revealed that chlorophyllides composites modulated DEGs that are associated with the endocrine system in MCF-7 cells and with the nervous system in MDA-MB-231 cells, respectively. The expression levels of 9 genes were validated by quantitative reverse transcription PCR (RT-qPCR). The expression of CCR1, STIM2, ETNK1, MAGl1 and TOP2A were upregulated in both chlorophyllides composites treated-MCF-7 and MDA-MB-231 cells. The different expression of NLRC5, SLC7A7 and PKN1 provided valuable information for future investigation and development of novel cancer therapy. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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Review

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30 pages, 3647 KiB

Open AccessReview

Structure–Activity Relationships in NHC–Silver Complexes as Antimicrobial Agents

by Luisa Ronga, Mario Varcamonti and Diego Tesauro

Molecules 2023, 28(11), 4435; https://doi.org/10.3390/molecules28114435 - 30 May 2023

Cited by 3 | Viewed by 1633

Abstract

Silver has a long history of antimicrobial activity and received an increasing interest in last decades owing to the rise in antimicrobial resistance. The major drawback is the limited duration of its antimicrobial activity. The broad-spectrum silver containing antimicrobial agents are well represented [...] Read more.

Silver has a long history of antimicrobial activity and received an increasing interest in last decades owing to the rise in antimicrobial resistance. The major drawback is the limited duration of its antimicrobial activity. The broad-spectrum silver containing antimicrobial agents are well represented by N-heterocyclic carbenes (NHCs) silver complexes. Due to their stability, this class of complexes can release the active Ag⁺ cations in prolonged time. Moreover, the properties of NHC can be tuned introducing alkyl moieties on N-heterocycle to provide a range of versatile structures with different stability and lipophilicity. This review presents designed Ag complexes and their biological activity against Gram-positive, Gram-negative bacteria and fungal strains. In particular, the structure–activity relationships underlining the major requirements to increase the capability to induce microorganism death are highlighted here. Moreover, some examples of encapsulation of silver–NHC complexes in polymer-based supramolecular aggregates are reported. The targeted delivery of silver complexes to the infected sites will be the most promising goal for the future. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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19 pages, 3028 KiB

Open AccessReview

The Challenging Treatment of Cisplatin-Resistant Tumors: State of the Art and Future Perspectives

by Giulia Coffetti, Martina Moraschi, Giorgio Facchetti and Isabella Rimoldi

Molecules 2023, 28(8), 3407; https://doi.org/10.3390/molecules28083407 - 12 Apr 2023

Cited by 7 | Viewed by 1619

Abstract

One of the main problems in chemotherapy using platinum drugs as anticancer agents is the resistance phenomenon. Synthesizing and evaluating valid alternative compounds is challenging. This review focuses on the last two years of progress in the studies of platinum (II)- and platinum [...] Read more.

One of the main problems in chemotherapy using platinum drugs as anticancer agents is the resistance phenomenon. Synthesizing and evaluating valid alternative compounds is challenging. This review focuses on the last two years of progress in the studies of platinum (II)- and platinum (IV)-based anticancer complexes. In particular, the research studies reported herein focus on the capability of some platinum-based anticancer agents to bypass resistance to chemotherapy, which is typical of well-known drugs such as cisplatin. Regarding platinum (II) complexes, this review deals with complexes in trans conformation; complexes containing bioactive ligands, as well as those that are differently charged, all experience a different reaction mechanism compared with cisplatin. Regarding platinum (IV) compounds, the focus was on complexes with biologically active ancillary ligands that exert a synergistic effect with platinum (II)-active complexes upon reduction, or those for which controllable activation can be realized thanks to intracellular stimuli. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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33 pages, 9861 KiB

Open AccessReview

Recent Trends in the Development of Novel Metal-Based Antineoplastic Drugs

by Lozan Todorov and Irena Kostova

Molecules 2023, 28(4), 1959; https://doi.org/10.3390/molecules28041959 - 18 Feb 2023

Cited by 15 | Viewed by 1978

Abstract

Since the accidental discovery of the anticancer properties of cisplatin more than half a century ago, significant efforts by the broad scientific community have been and are currently being invested into the search for metal complexes with antitumor activity. Coordination compounds of transition [...] Read more.

Since the accidental discovery of the anticancer properties of cisplatin more than half a century ago, significant efforts by the broad scientific community have been and are currently being invested into the search for metal complexes with antitumor activity. Coordination compounds of transition metals such as platinum (Pt), ruthenium (Ru) and gold (Au) have proven their effectiveness as diagnostic and/or antiproliferative agents. In recent years, experimental work on the potential applications of elements including lanthanum (La) and the post-transition metal gallium (Ga) in the field of oncology has been gaining traction. The authors of the present review article aim to help the reader “catch up” with some of the latest developments in the vast subject of coordination compounds in oncology. Herewith is offered a review of the published scientific literature on anticancer coordination compounds of Pt, Ru, Au, Ga and La that has been released over the past three years with the hope readers find the following article informative and helpful. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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33 pages, 10315 KiB

Open AccessReview

Highlights of New Strategies to Increase the Efficacy of Transition Metal Complexes for Cancer Treatments

by Ester Giorgi, Francesca Binacchi, Carlo Marotta, Damiano Cirri, Chiara Gabbiani and Alessandro Pratesi

Molecules 2023, 28(1), 273; https://doi.org/10.3390/molecules28010273 - 29 Dec 2022

Cited by 10 | Viewed by 2108

Abstract

Although important progress has been made, cancer still remains a complex disease to treat. Serious side effects, the insurgence of resistance and poor selectivity are some of the problems associated with the classical metal-based anti-cancer therapies currently in clinical use. New treatment approaches [...] Read more.

Although important progress has been made, cancer still remains a complex disease to treat. Serious side effects, the insurgence of resistance and poor selectivity are some of the problems associated with the classical metal-based anti-cancer therapies currently in clinical use. New treatment approaches are still needed to increase cancer patient survival without cancer recurrence. Herein, we reviewed two promising—at least in our opinion—new strategies to increase the efficacy of transition metal-based complexes. First, we considered the possibility of assembling two biologically active fragments containing different metal centres into the same molecule, thus obtaining a heterobimetallic complex. A critical comparison with the monometallic counterparts was done. The reviewed literature has been divided into two groups: the case of platinum; the case of gold. Secondly, the conjugation of metal-based complexes to a targeting moiety was discussed. Particularly, we highlighted some interesting examples of compounds targeting cancer cell organelles according to a third-order targeting approach, and complexes targeting the whole cancer cell, according to a second-order targeting strategy. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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30 pages, 1774 KiB

Open AccessReview

Metallo-Drugs in Cancer Therapy: Past, Present and Future

by Roxana Liana Lucaciu, Adriana Corina Hangan, Bogdan Sevastre and Luminița Simona Oprean

Molecules 2022, 27(19), 6485; https://doi.org/10.3390/molecules27196485 - 01 Oct 2022

Cited by 49 | Viewed by 3727

Abstract

Cancer treatments which include conventional chemotherapy have not proven very successful in curing human malignancies. The failures of these treatment modalities include inherent resistance, systemic toxicity and severe side effects. Out of 50% patients administrated to chemotherapy, only 5% survive. For these reasons, [...] Read more.

Cancer treatments which include conventional chemotherapy have not proven very successful in curing human malignancies. The failures of these treatment modalities include inherent resistance, systemic toxicity and severe side effects. Out of 50% patients administrated to chemotherapy, only 5% survive. For these reasons, the identification of new drug designs and therapeutic strategies that could target cancer cells while leaving normal cells unaffected still continues to be a challenge. Despite advances that have led to the development of new therapies, treatment options are still limited for many types of cancers. This review provides an overview of platinum, copper and ruthenium metal based anticancer drugs in clinical trials and in vitro/in vivo studies. Presumably, copper and ruthenium complexes have greater potential than Pt(II) complexes, showing reduced toxicity, a new mechanism of action, a different spectrum of activity and the possibility of non-cross-resistance. We focus the discussion towards past, present and future aspects. Full article

(This article belongs to the Special Issue Metal-Based Drugs: Past, Present and Future)

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