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Pharmaceutics
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Pharmaceutical Applications of Metal Complexes and Derived Materials
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Pharmaceutical Applications of Metal Complexes and Derived Materials

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

Deadline for manuscript submissions: 20 June 2025 | Viewed by 6632

Special Issue Editor

Prof. Dr. Pedro Ivo da Silva Maia

E-Mail Website
Guest Editor
Núcleo de Desenvolvimento de Compostos Bioativos (NDCBio), Universidade Federal do Triângulo Mineiro, Av. Dr. Randolfo Borges 1400, Uberaba 38025-440, MG, Brazil
Interests: basic chemistry of d and f-block elements; synthesis of bioactive ligands; metals in medicine; nuclear medicine; nanomaterials; new catalysts; biosensors; determination of crystal structures by single-crystal X-ray diffraction; mechanism of action of bioactive compounds

Special Issue Information

Dear Colleagues,

In recent years, Medicinal Inorganic Chemistry has demonstrated remarkable capacity in the development of metal complexes and related materials with innumerous pharmaceutical applications, encompassing therapeutic, diagnostic and theranostic purposes. The coordination of biologically active organic molecules and preparation of metallo-bionanomaterials has been used as a strategy to circumvent many of the difficulties associated with current chemotherapies, such as high toxicity, lack of activity during the chronic phase and cellular and microbial resistances. For the precise diagnosis of cancer and other diseases, considerable efforts have been made to develop more effective therapies, molecular imaging technologies and electronic devices which are based on the singular properties of metal complexes, such as the luminescent and magnetic, participation in redox processes and radiolabeling using metal radioisotopes. 

In this Special Issue, all contributions (original or review) on novel biologically active coordination compounds and related materials employed as pharmacological tools, including reports on their synthesis and characterization; preparation of biosensors; radiolabeling of ligands; biochemical/pharmacological evaluation and incorporation in drug delivery systems; as well as investigations of their biological targets, are welcome. Studies concerning known compounds, comprising analytical and computational investigations, are also encouraged provided there is a clear benefit to the field of Medicinal Chemistry.

Prof. Dr. Pedro Ivo da Silva Maia
Guest Editor

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Keywords

  • metallodrugs
  • metal complexes in cancer treatment
  • metal complexes as antimicrobial agents
  • delivery systems containing metal complexes
  • metal complexes in photodynamic therapy
  • metal complexes in biosensors
  • metal complexes as biomarkers
  • radiopharmaceuticals
  • computational studies in metallodrugs development
  • mechanism of action of bioactive metal complexes

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Published Papers (5 papers)

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Research

20 pages, 2006 KiB  
Article
99mTc-Labeled Diarylpyrazoles for Single-Emission Computer Tomography Imaging of Neurotensin Receptor-Positive Tumors: A Comparative Preclinical Study
by Roman Potemkin, Simone Maschauer, Harald Hübner, Torsten Kuwert, Tobias Bäuerle, Peter Gmeiner and Olaf Prante
Pharmaceutics 2025, 17(6), 700; https://doi.org/10.3390/pharmaceutics17060700 - 27 May 2025
Viewed by 312
Abstract
Background/Objectives: Neurotensin receptors (NTSRs), members of the G protein-coupled receptor (GPCR) family, have been found to be overexpressed in several types of human cancers, including breast, colon, lung, liver, prostate, and pancreatic cancer. In particular, NTSR1 is overexpressed in at least 75% of [...] Read more.
Background/Objectives: Neurotensin receptors (NTSRs), members of the G protein-coupled receptor (GPCR) family, have been found to be overexpressed in several types of human cancers, including breast, colon, lung, liver, prostate, and pancreatic cancer. In particular, NTSR1 is overexpressed in at least 75% of pancreatic ductal adenocarcinomas. The aim of the present study was the development and evaluation of new 99mTc-labeled nonpeptide NTSR1-antagonists for SPECT imaging of NTSR-positive tumors. Methods: Multistep syntheses of NTSR1 antagonist derivatives were performed following our previously described procedure. Two different chelating strategies were applied for 99mTc radiolabeling to provide the [99mTc]Tc-HYNIC complex [99mTc]1 and the [99mTc]Tc-tricarbonyl complex [99mTc]2. Receptor binding assays were performed using hNTSR1-expressing CHO cells. Radiochemical yields (RCYs) were determined by radio-HPLC. For [99mTc]1 and [99mTc]2, log D7.4, plasma protein binding, stability in human plasma and serum, and cellular uptake in HT-29 cells were determined. Biodistribution studies and small animal SPECT studies were performed in HT-29 tumor-bearing nude mice. Results: The radiosynthesis of [99mTc]1 (log D7.4 = −0.27) and [99mTc]2 (log D7.4 = 1.00) was successfully performed with RCYs of 94–96% (decay-corrected). Both radioligands were stable in human serum and plasma, showed plasma protein binding of 72% ([99mTc]1) and 82% ([99mTc]2), and exhibited high and specific uptake in HT-29 cells. Biodistribution studies in HT-29 tumor-bearing mice showed a higher tumor accumulation of [99mTc]1 compared to [99mTc]2 (8.8 ± 3.4 %ID/g vs. 2.7 ± 0.2 %ID/g at 2 h p.i.). [99mTc]2 showed exceptionally high intestinal accumulation (49 ± 22 %ID/g at 1 h p.i.) and was therefore considered unfavorable. In the SPECT/CT imaging of HT-29 tumor xenografts, [99mTc]1 showed a higher NTSR1-specific tumor uptake than [99mTc]2 at all time points after tracer injection, with 12 ± 2.8 %ID/g for [99mTc]1 vs. 3.1 ± 1.1 %ID/g for [99mTc]2 at 4 h p.i. and adequate tumor-to-background ratios. Conclusions: In particular, the [99mTc]Tc-HYNIC ligand ([99mTc]1) showed promising preclinical results, being a potential candidate for SPECT imaging and, therefore, appropriate for translation into the clinic. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Metal Complexes and Derived Materials)
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16 pages, 2433 KiB  
Article
[99mTc]Technetium and Rhenium Dithiocarbazate Complexes: Chemical Synthesis and Biological Assessment
by André Gustavo de Araujo Fernandes, Alyne Eloise Lafratta, Carolina Portela Luz, Debora Levy, Daniele de Paula Faria, Carlos Alberto Buchpiguel, Ulrich Abram, Victor Marcelo Deflon and Fabio Luiz Navarro Marques
Pharmaceutics 2025, 17(1), 100; https://doi.org/10.3390/pharmaceutics17010100 - 13 Jan 2025
Viewed by 1102
Abstract
Background/Objectives: Dithiocarbazates (DTCs) and their metal complexes have been studied regarding their property as anticancer activities. In this work, using S-benzyl-5-hydroxy-3-methyl-5-phenyl-4,5-dihydro-1H-pirazol-1-carbodithionate (H2bdtc), we prepared [ReO(bdtc)(Hbdtc)] and [[99mTc]TcO(bdtc)(Hbdtc)] complexes for tumor uptake and animal biodistribution studies. Methods: Re complex was [...] Read more.
Background/Objectives: Dithiocarbazates (DTCs) and their metal complexes have been studied regarding their property as anticancer activities. In this work, using S-benzyl-5-hydroxy-3-methyl-5-phenyl-4,5-dihydro-1H-pirazol-1-carbodithionate (H2bdtc), we prepared [ReO(bdtc)(Hbdtc)] and [[99mTc]TcO(bdtc)(Hbdtc)] complexes for tumor uptake and animal biodistribution studies. Methods: Re complex was prepared by a reaction of H2bdtc and (NBu4)[ReOCl4], the final product was characterized by IR, 1H NMR, CHN, and MS-ESI. 99mTc complex was prepared by the reaction of H2bdtc and [[99mTc]TcO4− and analyzed by planar and HPLC radiochromatography, and the stability was evaluated against amino acids and plasma. Biodistribution was performed in C57B/6 mice with B16F10 and TM1M implanted tumor. Results: Re is asymmetric coordinated by two dithiocarbazate ligands, one with O,N,S chelation, and the other with N,S chelation; [[99mTc]TcO(bdtc)(Hbdtc)] was prepared with a radiochemical yield of around 93%. The radioactive complex is hydrophobic (LogP = 1.03), stable for 6 h in PBS and L-histidine solution; stable for 1 h in plasma, but unstable in the presence of L-cysteine. Ex vivo biodistribution demonstrated that the compound has a fast and persistent (until 2 h) uptake by the spleen (55.46%), and tumor B16F10 and TM1M uptake is lower than 1%. In vivo SPECT/CT imaging confirmed ex vivo biodistribution, except by heterogenous TM1M accumulation but not in the B16-F10 lineage. Conclusions: H2bdtc proved to be an interesting chelator for rhenium or [99mTc]technetium. The right spleen uptake opened the opportunity to deepen the study of the molecule in this tissue and justifies future studies to identify the reason of heterogenous uptake in TM1M tumor uptake. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Metal Complexes and Derived Materials)
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24 pages, 6883 KiB  
Article
Organic Moiety on Sn(IV) Does Matter for In Vitro Mode of Action: nBu3Sn(IV) Compounds with Carboxylato N-Functionalized 2-Quinolones Induce Anoikis-like Cell Death in A375 Cells
by Marijana P. Kasalović, Sanja Jelača, Dušan Dimić, Danijela Maksimović-Ivanić, Verica V. Jevtić, Sanja Mijatović, Tobias Rüffer, Goran N. Kaluđerović and Nebojša Đ. Pantelić
Pharmaceutics 2024, 16(12), 1529; https://doi.org/10.3390/pharmaceutics16121529 - 28 Nov 2024
Viewed by 907
Abstract
Objectives: New tributyltin(IV) complexes containing the carboxylate ligands 3-(4-methyl-2-oxoquinolin-1(2H)-yl)propanoic acid (HL1) and 2-(4-methyl-2-oxoquinolin-1(2H)-yl)acetic acid (HL2) have been synthesized. Methods: Their structures have been determined by elemental microanalysis, FT-IR and multinuclear NMR (1H, 13C and 119Sn) [...] Read more.
Objectives: New tributyltin(IV) complexes containing the carboxylate ligands 3-(4-methyl-2-oxoquinolin-1(2H)-yl)propanoic acid (HL1) and 2-(4-methyl-2-oxoquinolin-1(2H)-yl)acetic acid (HL2) have been synthesized. Methods: Their structures have been determined by elemental microanalysis, FT-IR and multinuclear NMR (1H, 13C and 119Sn) spectroscopy and X-ray diffraction study. A solution state NMR analysis reveals a four-coordinated tributyltin(IV) complex in non-polar solvents, while an X-Ray crystallographic analysis confirms a five-coordinated trigonal-bipyramidal geometry around the tin atom due to the formation of 1D chains. A theoretical structural analysis was performed by optimization employing B3LYP-D3BJ functional and 6-311++G(d,p)/def2-TZVP(Sn) basis sets for H, C, N, O/Sn, respectively. The interactions between tin(IV) and surrounding atoms were examined by QTAIM approach. The in vitro antiproliferative activity of the synthesized compounds was evaluated by MTT and CV assays versus MCF-7 (human breast adenocarcinoma), HCT116 (human colorectal carcinoma), A375 (human melanoma), 4T1 (mouse breast carcinoma), CT26 (mouse colon carcinoma) and B16 (mouse melanoma) tumor cell lines. Results: Both synthesized compounds (nBu3SnL1 and nBu3SnL2) exerted powerful micromolar IC50 cytotoxicity values and demonstrated high selectivity toward malignant cells. Both experimental drugs affected cell adhesion and induced anchorage independent apoptosis, a favorable type of cell death with an essential role in cancer dissemination prevention. The BSA-binding affinity of the obtained organotin compounds was followed by spectrofluorometric titration and molecular docking simulations. Conclusions: The tributyltin(IV) compounds selectively induce anoikis-like cell death in A375 cells, also highlighting the importance of the organic moiety on the tin(IV) ion in the mechanism of action. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Metal Complexes and Derived Materials)
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14 pages, 7934 KiB  
Article
Induction of Non-Canonical Ferroptosis by Targeting Clusters Suppresses Glioblastoma
by Kai Cao, Liyuan Xue, Kaidi Luo, Wendi Huo, Panpan Ruan, Dongfang Xia, Xiuxiu Yao, Wencong Zhao, Liang Gao and Xueyun Gao
Pharmaceutics 2024, 16(9), 1205; https://doi.org/10.3390/pharmaceutics16091205 - 13 Sep 2024
Cited by 1 | Viewed by 1464
Abstract
Glioblastoma multiforme (GBM) is the most aggressive brain tumor. There is a pressing need to develop novel treatment strategies due to the poor targeting effect of current therapeutics. Here, a gold cluster coated with optimized GBM-targeting peptide is engineered, namely NA. NA can [...] Read more.
Glioblastoma multiforme (GBM) is the most aggressive brain tumor. There is a pressing need to develop novel treatment strategies due to the poor targeting effect of current therapeutics. Here, a gold cluster coated with optimized GBM-targeting peptide is engineered, namely NA. NA can efficiently target GBM both in vitro and in vivo. Interestingly, the uptake of NA significantly sensitizes GBM cells to ferroptosis, a form of programmed cell death that can bypass the tumor resistance to apoptosis. This effect is exerted through regulating the HO-1-dependent iron ion metabolism, which is the non-canonical pathway of ferroptosis. The combined treatment of a ferroptosis inducer and NA profoundly inhibited tumor growth in both the GBM spheroid model and a syngeneic mouse model with enhanced ferroptosis levels and excellent biosafety. Importantly, the infiltration of tumoricidal lymphocytes is also significantly increased within tumor. Therefore, NA presents a potential novel nanomaterial-based strategy for GBM treatment. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Metal Complexes and Derived Materials)
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28 pages, 3797 KiB  
Article
Gold(I) and Silver(I) Complexes Containing Hybrid Sulfonamide/Thiourea Ligands as Potential Leishmanicidal Agents
by Alice P. Borges, Malu M. S. Obata, Silvia H. Libardi, Rafael O. Trevisan, Victor M. Deflon, Ulrich Abram, Francis B. Ferreira, Luiz Antônio S. Costa, Antonio O. T. Patrocínio, Marcos V. da Silva, Júlio C. Borges and Pedro I. S. Maia
Pharmaceutics 2024, 16(4), 452; https://doi.org/10.3390/pharmaceutics16040452 - 25 Mar 2024
Cited by 3 | Viewed by 1805
Abstract
Leishmaniasis is a group of parasitic diseases with the potential to infect more than 1 billion people; however, its treatment is still old and inadequate. In order to contribute to changing this view, this work consisted of the development of complexes derived from [...] Read more.
Leishmaniasis is a group of parasitic diseases with the potential to infect more than 1 billion people; however, its treatment is still old and inadequate. In order to contribute to changing this view, this work consisted of the development of complexes derived from MI metal ions with thioureas, aiming to obtain potential leishmanicidal agents. The thiourea ligands (HLR) were obtained by reactions of p-toluenesulfohydrazide with R-isothiocyanates and were used in complexation reactions with AgI and AuI, leading to the formation of complexes of composition [M(HLR)2]X (M = Ag or Au; X = NO3− or Cl−). All compounds were characterized by FTIR, 1H NMR, UV-vis, emission spectroscopy and elemental analysis. Some representatives were additionally studied by ESI-MS and single-crystal XRD. Their properties were further analyzed by DFT calculations. Their cytotoxicity on Vero cells and the extracellular leishmanicidal activity on Leishmania infantum and Leishmania braziliensis cells were evaluated. Additionally, the interaction of the complexes with the Old Yellow enzyme of the L. braziliensis (LbOYE) was examined. The biological tests showed that some compounds present remarkable leishmanicidal activity, even higher than that of the standard drug Glucantime, with different selectivity for the two species of Leishmania. Finally, the interaction studies with LbOYE revealed that this enzyme could be one of their biological targets. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Metal Complexes and Derived Materials)
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