{"title":"Trans-Pd(II) complexes: A different approach for the development of promising anticancer drugs","authors":"Ester Giorgi , Francesca Binacchi , Michele Mannelli , Damiano Cirri , Andrea Cesari , Matteo Boldrini , Carlo Marotta , Claudia Ghelarducci , Diletta Corvaglia , Fabio Bellina , Tania Gamberi , Alessandro Pratesi , Chiara Gabbiani","doi":"10.1016/j.ica.2025.122645","DOIUrl":null,"url":null,"abstract":"<div><div>Pd(II) complexes, thanks to the similarity of their coordination chemistry to that of Pt(II) compounds and their improved solubility in water than the latter, offer a promising way for the design of novel anticancer agents. Considering that <em>trans</em>-Pd(II) complexes are more cytotoxic than their <em>cis</em>-counterparts and endowing them with ligands that could grant them improved stabilization during their circulation inside the body, a panel of <em>trans</em>-Pd(II) complexes with general formula <em>trans</em>-PdL<sub>2</sub>X<sub>2</sub> (where L = pyridine or piperidine, X = Cl, Br, I) was synthesized. The interactions of these complexes with model proteins were studied with UV–vis and NMR spectroscopy, and their <em>in vitro</em> activity against selected cancer cell lines was also investigated. The study demonstrates that square-planar trans-Pd(II) complexes have potential as chemical tools in medicinal chemistry. They are able to interact with proteomic targets, and despite their limited cytotoxic activity towards the selected tumor cell lines, the interaction profiles and solution reactivity provide valuable mechanistic insights on the mode of action of this class of compounds. Indeed, a reproducible and accessible methodology was defined to investigate the square-planar <em>trans</em>-Pd(II) complexes.</div></div>","PeriodicalId":13599,"journal":{"name":"Inorganica Chimica Acta","volume":"581 ","pages":"Article 122645"},"PeriodicalIF":2.7000,"publicationDate":"2025-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Inorganica Chimica Acta","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0020169325001112","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, INORGANIC & NUCLEAR","Score":null,"Total":0}
引用次数: 0
Abstract
Pd(II) complexes, thanks to the similarity of their coordination chemistry to that of Pt(II) compounds and their improved solubility in water than the latter, offer a promising way for the design of novel anticancer agents. Considering that trans-Pd(II) complexes are more cytotoxic than their cis-counterparts and endowing them with ligands that could grant them improved stabilization during their circulation inside the body, a panel of trans-Pd(II) complexes with general formula trans-PdL2X2 (where L = pyridine or piperidine, X = Cl, Br, I) was synthesized. The interactions of these complexes with model proteins were studied with UV–vis and NMR spectroscopy, and their in vitro activity against selected cancer cell lines was also investigated. The study demonstrates that square-planar trans-Pd(II) complexes have potential as chemical tools in medicinal chemistry. They are able to interact with proteomic targets, and despite their limited cytotoxic activity towards the selected tumor cell lines, the interaction profiles and solution reactivity provide valuable mechanistic insights on the mode of action of this class of compounds. Indeed, a reproducible and accessible methodology was defined to investigate the square-planar trans-Pd(II) complexes.
期刊介绍:
Inorganica Chimica Acta is an established international forum for all aspects of advanced Inorganic Chemistry. Original papers of high scientific level and interest are published in the form of Articles and Reviews.
Topics covered include:
• chemistry of the main group elements and the d- and f-block metals, including the synthesis, characterization and reactivity of coordination, organometallic, biomimetic, supramolecular coordination compounds, including associated computational studies;
• synthesis, physico-chemical properties, applications of molecule-based nano-scaled clusters and nanomaterials designed using the principles of coordination chemistry, as well as coordination polymers (CPs), metal-organic frameworks (MOFs), metal-organic polyhedra (MPOs);
• reaction mechanisms and physico-chemical investigations computational studies of metalloenzymes and their models;
• applications of inorganic compounds, metallodrugs and molecule-based materials.
Papers composed primarily of structural reports will typically not be considered for publication.