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Polyamine Drug Discovery
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Polyamine Drug Discovery

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (29 February 2024) | Viewed by 13410

Special Issue Editors

Prof. Dr. Anna Mìnarini

E-Mail Website
Guest Editor
Department of Pharmacy and Biotechnology, Alma Mater Studiorum Università di Bologna, Bologna, Italy
Interests: medicinal chemistry; drug discovery; synthesis and structure–activity relationships of biologically active compounds; multitarget agents; hybrid compounds; polyamine analogues; polyamine conjugates; anticancer agents; amino oxidase inhibitors; neuroprotective agents; antioxidant molecules
Prof. Dr. Michela Rosini

E-Mail Website
Guest Editor
Department of Pharmacy & Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
Interests: Design and synthesis of small molecules as probes for the investigation of biological processes or as drug candidates for neurodegenerative diseases and cancer

Special Issue Information

Dear Colleagues,

Naturally occurring polyamines as well as synthetic polyamines affect various biological pathways through either activation or inhibition of these pathways. This indicates that polyamine research has a great potential in drug discovery for the treatment of different diseases. Many notable findings in this field have been concerned with the identification of polyamine analogues as chemopreventive and antiproliferative agents, antiparasitic compounds, neuroprotectants, and neurotransmitter receptor agonists/antagonists.

This Special Issue “Polyamines in Drug Discovery” welcomes the submission of review and research articles related to the design, synthesis, and pharmacological characterization of new polyamine-based molecules that could underlie innovative approaches in drug development, for example, by targeting polyamine metabolism and transport or by acting as epigenetic modulators.

Prof. Dr. Anna Mìnarini
Prof. Dr. Michela Rosini
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 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 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 2700 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

  • anticancer agents;
  • synthetic polyamines;
  • polyamine conjugates;
  • polyamine transport system;
  • polyamine oxidase modulators;
  • antiparasitic compounds;
  • chemoprevention;
  • neuroprotectants;
  • monoamine oxidase inhibitors;
  • epigenetic targets.

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Published Papers (4 papers)

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Research

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21 pages, 3456 KiB  
Article
Antimicrobial Properties of New Polyamines Conjugated with Oxygen-Containing Aromatic Functional Groups
by Mario Inclán, Neus Torres Hernández, Alejandro Martínez Serra, Gonzalo Torrijos Jabón, Salvador Blasco, Cecilia Andreu, Marcel lí del Olmo, Beatriz Jávega, José-Enrique O’Connor and Enrique García-España
Molecules 2023, 28(22), 7678; https://doi.org/10.3390/molecules28227678 - 20 Nov 2023
Cited by 2 | Viewed by 2182
Abstract
Antibiotic resistance is now a first-order health problem, which makes the development of new families of antimicrobials imperative. These compounds should ideally be inexpensive, readily available, highly active, and non-toxic. Here, we present the results of our investigation regarding the antimicrobial activity of [...] Read more.
Antibiotic resistance is now a first-order health problem, which makes the development of new families of antimicrobials imperative. These compounds should ideally be inexpensive, readily available, highly active, and non-toxic. Here, we present the results of our investigation regarding the antimicrobial activity of a series of natural and synthetic polyamines with different architectures (linear, tripodal, and macrocyclic) and their derivatives with the oxygen-containing aromatic functional groups 1,3-benzodioxol, ortho/para phenol, or 2,3-dihydrobenzofuran. The new compounds were prepared through an inexpensive process, and their activity was tested against selected strains of yeast, as well as Gram-positive and Gram-negative bacteria. In all cases, the conjugated derivatives showed antimicrobial activity higher than the unsubstituted polyamines. Several factors, such as the overall charge at physiological pH, lipophilicity, and the topology of the polyamine scaffold were relevant to their activity. The nature of the lipophilic moiety was also a determinant of human cell toxicity. The lead compounds were found to be bactericidal and fungistatic, and they were synergic with the commercial antifungals fluconazole, cycloheximide, and amphotericin B against the yeast strains tested. Full article
(This article belongs to the Special Issue Polyamine Drug Discovery)
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27 pages, 73035 KiB  
Article
Solid-Phase Synthesis of Selectively Mono-Fluorobenz(o)ylated Polyamines as a Basis for the Development of 18F-Labeled Radiotracers
by Robert Wodtke, Jens Pietzsch and Reik Löser
Molecules 2021, 26(22), 7012; https://doi.org/10.3390/molecules26227012 - 20 Nov 2021
Cited by 1 | Viewed by 2697
Abstract
Polyamines are highly attractive vectors for tumor targeting, particularly with regards to the development of radiolabeled probes for imaging by positron emission (PET) and single-photon emission computed tomography (SPECT). However, the synthesis of selectively functionalized derivatives remains challenging due to the presence of [...] Read more.
Polyamines are highly attractive vectors for tumor targeting, particularly with regards to the development of radiolabeled probes for imaging by positron emission (PET) and single-photon emission computed tomography (SPECT). However, the synthesis of selectively functionalized derivatives remains challenging due to the presence of multiple amino groups of similar reactivity. In this work, we established a synthetic methodology for the selective mono-fluorobenz(o)ylation of various biogenic diamines and polyamines as lead compounds for the perspective development of substrate-based radiotracers for targeting polyamine-specific membrane transporters and enzymes such as transglutaminases. For this purpose, the polyamine scaffold was constructed by solid-phase synthesis of the corresponding oxopolyamines and subsequent reduction with BH3/THF. Primary and secondary amino groups were selectively protected using Dde and Boc as protecting groups, respectively, in orientation to previously reported procedures, which enabled the selective introduction of the reporter groups. For example, N1-FBz-spermidine, N4-FBz-spermidine, N8-FBz-spermidine, and N1-FBz-spermine and N4-FBz-spermine (FBz = 4-fluorobenzoyl) were obtained in good yields by this approach. The advantages and disadvantages of this synthetic approach are discussed in detail and its suitability for radiolabeling was demonstrated for the solid-phase synthesis of N1-[18F]FBz-cadaverine. Full article
(This article belongs to the Special Issue Polyamine Drug Discovery)
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Review

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30 pages, 3888 KiB  
Review
Polyamine–Drug Conjugates: Do They Boost Drug Activity?
by Filippo Basagni, Giambattista Marotta, Michela Rosini and Anna Minarini
Molecules 2023, 28(11), 4518; https://doi.org/10.3390/molecules28114518 - 2 Jun 2023
Cited by 3 | Viewed by 2071
Abstract
Over the past two decades, the strategy of conjugating polyamine tails with bioactive molecules such as anticancer and antimicrobial agents, as well as antioxidant and neuroprotective scaffolds, has been widely exploited to enhance their pharmacological profile. Polyamine transport is elevated in many pathological [...] Read more.
Over the past two decades, the strategy of conjugating polyamine tails with bioactive molecules such as anticancer and antimicrobial agents, as well as antioxidant and neuroprotective scaffolds, has been widely exploited to enhance their pharmacological profile. Polyamine transport is elevated in many pathological conditions, suggesting that the polyamine portion could improve cellular and subcellular uptake of the conjugate via the polyamine transporter system. In this review, we have presented a glimpse on the polyamine conjugate scenario, classified by therapeutic area, of the last decade with the aim of highlighting achievements and fostering future developments. Full article
(This article belongs to the Special Issue Polyamine Drug Discovery)
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22 pages, 5913 KiB  
Review
Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications
by Artemiy Nichugovskiy, Gian Cesare Tron and Mikhail Maslov
Molecules 2021, 26(21), 6579; https://doi.org/10.3390/molecules26216579 - 30 Oct 2021
Cited by 10 | Viewed by 4748
Abstract
Biogenic polyamines (PAs) are involved in the growth and development of normal cells, and their intracellular concentration is stable. The concentration of PAs in cancer cells is significantly increased to promote and sustain their rapid proliferation. Over the years, synthetic PAs, which differ [...] Read more.
Biogenic polyamines (PAs) are involved in the growth and development of normal cells, and their intracellular concentration is stable. The concentration of PAs in cancer cells is significantly increased to promote and sustain their rapid proliferation. Over the years, synthetic PAs, which differ in their structure, have demonstrated high antitumor activity and are involved in clinical trials. The chemical synthesis of PAs and their conjugates require the correct choice of synthetic pathways—methods for constructing conjugates and the orthogonal protection of amino groups. The most common methods of synthesis of PA conjugates are acylation of regioselectively protected PAs or their alkylation under the conditions of the Fukuyama reaction. One of the most promising methods of PA synthesis is the use of a multicomponent Ugi reaction, which allows various PAs to be obtained in high yields. In this review, we describe and analyze various approaches that are used in the synthesis of polyamines and their conjugates. Full article
(This article belongs to the Special Issue Polyamine Drug Discovery)
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