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Molecules
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New Opportunities for Platinum-Based Anticancer Complexes
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New Opportunities for Platinum-Based Anticancer Complexes

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

Deadline for manuscript submissions: closed (15 September 2021) | Viewed by 4756

Special Issue Editors

Prof. Dr. Mauro Ravera

E-Mail Website
Guest Editor
Dipartimento di Scienze e Innovazione Tecnologica, Università del Piemonte Orientale, Viale Michel 11, 15121 Alessandria, Italy
Interests: bioinorganic chemistry; bioorganometallic chemistry; medicinal inorganic chemistry; biologically active transition metal complexes; metal-based (in particular, platinum) anticancer agents; drug targeting and delivery; inorganic electrochemistry
Special Issues, Collections and Topics in MDPI journals
Dr. Elisabetta Gabano

E-Mail Website
Guest Editor
Dipartimento per lo Sviluppo Sostenibile e la Transizione Ecologica, Università del Piemonte Orientale, Piazza S. Eusebio 5, 13100 Vercelli, Italy
Interests: bioinorganic chemistry; coordination compounds; Pt complexes as potential antitumor drugs; drug targeting and delivery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Despite the development of more targeted and less toxic drugs, traditional chemotherapy with platinum-based drugs is still one of the gold standard approaches for the treatment of cancer. The aim of this Special Issue is to collect and summarize new ideas and future trends in platinum-based complexes and materials, including compounds with bioactive ligands, multifunctional drugs, prodrugs, drug delivery systems, and theranostics metal complexes.

Prof. Dr. Mauro Ravera
Dr. Elisabetta Gabano
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

  • platinum-based drugs
  • platinum complexes
  • metal-based drugs
  • metallodrugs
  • metallopharmaceuticals
  • anticancer agents
  • chemotherapy
  • drug repositioning
  • coordination compounds with bioactive ligands
  • multifunctional drugs
  • prodrugs
  • drug delivery systems
  • theranostics metal complexes

Published Papers (2 papers)

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Research

17 pages, 1877 KiB  
Article
Unsymmetric Cisplatin-Based Pt(IV) Conjugates Containing a PARP-1 Inhibitor Pharmacophore Tested on Malignant Pleural Mesothelioma Cell Lines
by Elisabetta Gabano, Giulia Pinton, Cecilia Balzano, Sara Boumya, Domenico Osella, Laura Moro and Mauro Ravera
Molecules 2021, 26(16), 4740; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26164740 - 05 Aug 2021
Cited by 9 | Viewed by 2036
Abstract
Cisplatin is widely employed as a first-line chemotherapeutic agent for many solid tumors, including malignant pleural mesothelioma (MPM). However, its clinical use is limited by heavy side effects and acquired resistance, the latter being mainly related to enhanced DNA repair. Many clinical trials [...] Read more.
Cisplatin is widely employed as a first-line chemotherapeutic agent for many solid tumors, including malignant pleural mesothelioma (MPM). However, its clinical use is limited by heavy side effects and acquired resistance, the latter being mainly related to enhanced DNA repair. Many clinical trials using combinations of platinum drugs and PARP-1 inhibitors (PARPis) have been carried out, with the hope that such combinations might lead to improved therapeutic efficacy against tumors. Here, the synthesis and efficacy in reducing MPM cell viability of four cisplatin-based Pt(IV) prodrugs containing the PARPi 3-aminobenzamide (3-ABA) fragment are described. The most promising conjugate is more effective than cisplatin or cisplatin/3-ABA combination, administered in equimolar doses, in inhibiting PARP-1 activity and inducing apoptosis in BRCA1/2 wild type MPM cells, grown as monolayer or as multicellular spheroids. Full article
(This article belongs to the Special Issue New Opportunities for Platinum-Based Anticancer Complexes)
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20 pages, 4114 KiB  
Article
New Oxaliplatin-Pyrophosphato Analogs with Improved In Vitro Cytotoxicity
by Alessandra Barbanente, Rosa Maria Iacobazzi, Amalia Azzariti, James D. Hoeschele, Nunzio Denora, Paride Papadia, Concetta Pacifico, Giovanni Natile and Nicola Margiotta
Molecules 2021, 26(11), 3417; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26113417 - 04 Jun 2021
Cited by 4 | Viewed by 2099
Abstract
Two new Pt(II)-pyrophosphato complexes containing the carrier ligands cis-1,3-diaminocyclohexane (cis-1,3-DACH) and trans-1,2-diamine-4-cyclohexene (1,2-DACHEX), variants of the 1R,2R-diaminocyclohexane ligand present in the clinically used Pt-drug oxaliplatin, have been synthesized with the aim of developing new potential [...] Read more.
Two new Pt(II)-pyrophosphato complexes containing the carrier ligands cis-1,3-diaminocyclohexane (cis-1,3-DACH) and trans-1,2-diamine-4-cyclohexene (1,2-DACHEX), variants of the 1R,2R-diaminocyclohexane ligand present in the clinically used Pt-drug oxaliplatin, have been synthesized with the aim of developing new potential antitumor drugs with high bone tropism. The complexes are more stable at physiological pH than in acid conditions, with Na2[Pt(pyrophosphato)(cis-1,3-DACH)] (1) slightly more stable than [Pt(dihydrogenpyrophosphato)(1,2-DACHEX)] (2). The greater reactivity at acidic pH ensures a greater efficacy at the tumor site. Preliminary NMR studies indicate that 1 and 2 react slowly with 5’-GMP (used as a model of nucleic acids), releasing the pyrophosphate ligand and affording the bis 5’-GMP adduct. In vitro cytotoxicity assays performed against a panel of four human cancer cell lines have shown that both compounds are more active than oxaliplatin. Flow cytometry studies on HCT116 cells showed that the pyrophosphato compounds with the non-classical 1,3- and 1,4-diaminocyclohexane ligands (1 and 4) are the most capable to induce cells’ death by apoptosis and necrosis. Full article
(This article belongs to the Special Issue New Opportunities for Platinum-Based Anticancer Complexes)
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