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Special Issue "Metal-Based Drugs"

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: 31 December 2019

Special Issue Editors

Guest Editor
Prof. Dr. Carlo Santini

School of Science and Technology, Chemistry Division, University of Camerino, via Sant’Agostino 1, 62032 Camerino (MC), Italy
Website | E-Mail
Interests: metal-based drugs; coordination chemistry; functional metal complexes; hybrid materials; inorganic and organometallic chemistry; scorpionate ligands; phosphanes; N-heterocyclic carbenes
Guest Editor
Prof. Dr. Maura Pellei

School of Science and Technology, Chemistry Division, University of Camerino, via Sant’Agostino 1, 62032 Camerino (MC), Italy
Website | E-Mail
Phone: 0737402213
Interests: metal-based drugs; bioinorganic chemistry; coordination chemistry; inorganic materials; organometalllic chemistry; copper; scorpionate ligands; phosphanes N-heterocyclic carbenes

Special Issue Information

Dear Colleagues,

Metals have been considered for millennia to have medicinal values, and with the advent of modern medicine, numerous metal-based drugs have proven to be highly effective in clinical settings. Many different metal ions have shown activity against a range of diseases, beyond their well-known applications in cancer (cisplatin) or rheumatoid arthritis (auranofin). The widespread medicinal applications of metal-based compounds have captured the attention of the scientific community in recent years for the variety of compounds studied owing to their wide spectrum of reactivity and the width of their applications in medicinal chemistry for the synthesis of chemotherapeutic and diagnostic molecules not readily accessible to organic compounds.

This Special Issue will cover a selection of recent research and review articles to collect and disseminate some of the most significant and recent contributions in the field of metals used in medicine, highlighting their pharmacological applications in several diseases, such as cancers, diabetes, osteoporosis, and as diagnostic agents.

Prof. Dr. Carlo Santini
Prof. Dr. Maura Pellei
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 papers will be 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. Molecules is an international peer-reviewed open access semimonthly 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 1800 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

  • metals in medicine
  • coordination complexes
  • organometallics
  • anticancer agents
  • antibacterial agents
  • metal-based diagnostic agents
  • radiopharmaceuticals
  • chelation therapy
  • chemotherapy

Published Papers (4 papers)

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Research

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Open AccessArticle
Discovery of Cisplatin Binding to Thymine and Cytosine on a Single-Stranded Oligodeoxynucleotide by High Resolution FT-ICR Mass Spectrometry
Molecules 2019, 24(10), 1852; https://doi.org/10.3390/molecules24101852
Received: 16 April 2019 / Revised: 9 May 2019 / Accepted: 13 May 2019 / Published: 14 May 2019
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Abstract
The clinically widely-used anticancer drug, cisplatin, binds strongly to DNA as a DNA-damaging agent. Herein, we investigated the interaction of cisplatin with a 15-mer single-stranded C,T-rich oligodeoxynucleotide, 5′-CCTT4CTT7G8C9T10TCTCC-3′ (ODN15), using ultra-high resolution Fourier [...] Read more.
The clinically widely-used anticancer drug, cisplatin, binds strongly to DNA as a DNA-damaging agent. Herein, we investigated the interaction of cisplatin with a 15-mer single-stranded C,T-rich oligodeoxynucleotide, 5′-CCTT4CTT7G8C9T10TCTCC-3′ (ODN15), using ultra-high resolution Fourier transform ion cyclotron resonance mass spectrometry (FT-ICR MS) in conjunction with tandem mass spectrometry (top-down MS). Top-down MS analysis with collision-induced dissociation (CID) fragmentation of the mono-platinated and di-platinated ODN15 provided abundant and informative Pt-containing or Pt-free a/[a − B], w and internal fragments, allowing the unambiguous identification of T4, T7, C9, and T10 as the platination sites on the cisplatin-ODN15 adducts. These results revealed that, in addition to the well-established guanine site, the unexpected thermodynamic binding of cisplatin to cytosine and thymine bases was also evident at the oligonucleotide level. Furthermore, the binding models of cisplatin with cytosine and thymine bases were built as the Pt coordinated to cytosine-N(3) and thymine-N(3) with displacement of the proton or tautomerization of thymine. These findings contribute to a better understanding of the mechanism of action of cisplatin and its preference for gene loci when the drug binds to cellular DNA, and also demonstrate the great potential and superiority of FT-ICR MS in studying the interactions of metallodrugs with large biomolecules. Full article
(This article belongs to the Special Issue Metal-Based Drugs)
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Open AccessFeature PaperArticle
Syntheses and Biological Studies of Cu(II) Complexes Bearing Bis(pyrazol-1-yl)- and Bis(triazol-1-yl)-acetato Heteroscorpionate Ligands
Molecules 2019, 24(9), 1761; https://doi.org/10.3390/molecules24091761
Received: 6 April 2019 / Revised: 29 April 2019 / Accepted: 3 May 2019 / Published: 7 May 2019
PDF Full-text (2140 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Copper(II) complexes of bis(pyrazol-1-yl)- and bis(triazol-1-yl)-acetate heteroscorpionate ligands have been synthesized. The copper(II) complexes [HC(COOH)(pzMe2)2]Cu[HC(COO)(pzMe2)2]·ClO4, [HC(COOH)(pz)2]2Cu(ClO4)2 (pzMe2 = 3,5-dimethylpyrazole; pz = pyrazole) were prepared by [...] Read more.
Copper(II) complexes of bis(pyrazol-1-yl)- and bis(triazol-1-yl)-acetate heteroscorpionate ligands have been synthesized. The copper(II) complexes [HC(COOH)(pzMe2)2]Cu[HC(COO)(pzMe2)2]·ClO4, [HC(COOH)(pz)2]2Cu(ClO4)2 (pzMe2 = 3,5-dimethylpyrazole; pz = pyrazole) were prepared by the reaction of Cu(ClO4)2·6H2O with bis(3,5-dimethylpyrazol-1-yl)acetic acid (HC(COOH)(pzMe2)2) and bis(pyrazol-1-yl)acetic acid (HC(COOH)(pz)2) ligands in ethanol solution. The copper(II) complex [HC(COOH)(tz)2]2Cu(ClO4)2·CH3OH (tz = 1,2,4-triazole) was prepared by the reaction of Cu(ClO4)2·6H2O with bis(1,2,4-triazol-1-yl)acetic acid (HC(COOH)(tz)2) ligand in methanol solution. The synthesized Cu(II) complexes, as well as the corresponding uncoordinated ligands, were evaluated for their cytotoxic activity in monolayer and 3D spheroid cancer cell cultures with different Pt(II)-sensitivity. The results showed that [HC(COOH)(pzMe2)2]Cu[HC(COO)(pzMe2)2]·ClO4 was active against cancer cell lines derived from solid tumors at low IC50 and this effect was retained in the spheroid model. Structure and ultra-structure changes of treated cancer cells analyzed by Transmission Electron Microscopy (TEM) highlighted the induction of a cytoplasmic vacuolization, thus suggesting paraptotic-like cancer cell death triggering. Full article
(This article belongs to the Special Issue Metal-Based Drugs)
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Open AccessFeature PaperArticle
Effect of Manganese Chloride and of Cotreatment with Cadmium Chloride on the In Vitro Proliferative, Motile, and Invasive Behavior of MDA-MB231 Breast Cancer Cells
Molecules 2019, 24(7), 1205; https://doi.org/10.3390/molecules24071205
Received: 7 March 2019 / Revised: 21 March 2019 / Accepted: 25 March 2019 / Published: 27 March 2019
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Abstract
We examined the dose–response effect of MnCl2 on the proliferative behavior of triple-negative breast cancer MDA-M231 cells vs. immortalized HB2 cells from breast epithelium taken as nontumoral counterparts. We also tested the effect of MnCl2 on tumor cell invasiveness in vitro [...] Read more.
We examined the dose–response effect of MnCl2 on the proliferative behavior of triple-negative breast cancer MDA-M231 cells vs. immortalized HB2 cells from breast epithelium taken as nontumoral counterparts. We also tested the effect of MnCl2 on tumor cell invasiveness in vitro by evaluating the relative invasion indexes through Boyden chamber assays. Moreover, we checked whether cotreatment with both MnCl2 and CdCl2 could modify the observed biological response by MDA-MB231 cells. Our results show a promotional impact of MnCl2 on cell proliferation, with 5 µM concentration inducing the more pronounced increase after 96-h exposure, which is not shared by HB2 cells. Exposure to 5 µM MnCl2 induced also an elevation of the relative invasion index of cancer cells. The Mn-mediated stimulatory effects were counteracted by cotreatment with CdCl2. These data support the concept that human exposure to high environmental concentrations of Mn may increase the risk of carcinogenesis and metastasis by prompting the expansion and dissemination of triple-negative breast cancer cells. On the other hand, the Mn-counteracting anticancer property of Cd looks promising and deserves a more detailed characterization of the involved intracellular targets aimed to the molecular modeling of specific antineoplastic agents against malignant breast cancer spreading. Full article
(This article belongs to the Special Issue Metal-Based Drugs)
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Other

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Open AccessLetter
Interdisciplinary Tasks in the Cyclotron Production of Radiometals for Medical Applications. The Case of 47Sc as Example
Molecules 2019, 24(3), 444; https://doi.org/10.3390/molecules24030444
Received: 7 December 2018 / Revised: 22 January 2019 / Accepted: 24 January 2019 / Published: 26 January 2019
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Abstract
The growing number of cyclotrons of different sizes installed in the territory has given a strong impulse to the production of conventional and emerging radionuclides for medical applications. In particular, the great advantage of using medical cyclotrons is the possibility to produce on-site, [...] Read more.
The growing number of cyclotrons of different sizes installed in the territory has given a strong impulse to the production of conventional and emerging radionuclides for medical applications. In particular, the great advantage of using medical cyclotrons is the possibility to produce on-site, when needed (on-demand), with medical radionuclides of interest encouraging the personalized medicine approach. Radiometals satisfy the ideal characteristics that radionuclides should have for routine employment in nuclear medicine, especially since they have a robust chemistry suitable to synthetize stable in vivo radiopharmaceuticals with high radiochemical yields. In this letter several interdisciplinary aspects involved in the radiometals cyclotron production cycle are summarized focusing the attention on cyclotron production facilities, target material, and chemical processing available for medical applications. As an example, the current status and recent development in the production of the theranostic radionuclide scandium-47 have been reported. Full article
(This article belongs to the Special Issue Metal-Based Drugs)
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