130600 20240319081014.0 doi 10.1039/d2dt01963a sideral 130215 ART-2022-130215 eng Gascón, Elena Gold(I) metallocyclophosphazenes with antibacterial potency and antitumor efficacy. Synergistic antibacterial action of a heterometallic gold and silver-cyclophosphazene 2022 Access copy available to the general public Unrestricted One of the most important uses of phosphazenes today involves its biomedical applications. They can also be employed as scaffolds for the design and construction of a variety of ligands in order to coordinate them to metallic drugs. The coordination chemistry of the (amino)cyclotriphosphazene ligand, [N3P3(NHCy)6], towards gold(I) complexes has been studied. Neutral complexes, [N3P3(NHCy)6{AuX}n] (X = Cl or C6F5; n = 1 or 2) (1–4), cationic complexes, [N3P3(NHCy)6{Au(PR3)}n](NO3)n (PR3 = PPh3, PPh2Me, TPA; n = 1, 2 or 3) (6–12) [TPA = 1,3,5-triaza-7-phosphaadamantane] and a heterometallic compound [N3P3(NHCy)6{Au(PPh3)}2{Ag(PPh3)}](NO3)3 (13) have been obtained and characterized by various methods including single-crystal X-ray diffraction for 7, which confirms the coordination of gold atoms to the nitrogens of the phosphazene ring. Compounds 1, 4, 6–13 were screened for in vitro cytotoxic activity against two tumor human cell lines, MCF7 (breast adenocarcinoma) and HepG2 (hepatocellular carcinoma), and for antimicrobial activity against five bacterial species including Gram-positive, Gram-negative, and Mycobacteria. Both the median inhibitory concentration (IC50) and minimum inhibitory concentration (MIC) values are among the lowest found for any gold or silver derivatives against the cell lines and particularly against the Gram-positive (S. aureus) strain and the mycobacteria used in this work. Structure–activity relationships are discussed in order to determine the influence of ancillary ligands and the number and type of metal atoms (silver or gold). Compounds 4 and 8 showed not only maximal potency on human cells but also some tumour selectivity. Remarkably, compound 13, with both gold and silver atoms, showed outstanding activity against both Gram-positive and Gram-negative strains (nanomolar range), thus having a cooperative effect between gold and silver, with MIC values which are similar or lower than those of gentamicine, ciprofloxacin and rifampicine. The broad spectrum antimicrobial efficacy of all these metallophosphazenes and particularly of heterometallic compound 13 could be very useful to obtain materials for surfaces with antimicrobial properties that are increasingly in demand. info:eu-repo/grantAgreement/ES/DGA/B25-20R info:eu-repo/grantAgreement/ES/DGA/E47-20R info:eu-repo/grantAgreement/ES/DGA-FEDER/Construyendo Europa desde Aragón info:eu-repo/grantAgreement/ES/MINECO/MAT2017-84838-P info:eu-repo/semantics/openAccess All rights reserved http://www.europeana.eu/rights/rr-f/ 4.0 2022 CHEMISTRY, INORGANIC & NUCLEAR 7 / 42 = 0.167 2022 Q1 T1 0.79 2022 Inorganic Chemistry 2022 Q1 7.1 2022 info:eu-repo/semantics/article info:eu-repo/semantics/acceptedVersion Otal, Isabel Universidad de Zaragoza (orcid)0000-0003-1027-7583 Maisanaba, Sara Llana-Ruiz-Cabello, María Valero, Eva Repetto, Guillermo Jones, Peter G. Oriol, Luis Universidad de Zaragoza (orcid)0000-0002-0922-5615 Jiménez, Josefina Universidad de Zaragoza (orcid)0000-0002-3444-0851 2010 760 Universidad de Zaragoza Dpto. Química Inorgánica Área Química Inorgánica 1011 630 Universidad de Zaragoza Dpto. Microb.Ped.Radio.Sal.Pú. Área Microbiología 2013 765 Universidad de Zaragoza Dpto. Química Orgánica Área Química Orgánica 51, 36 (2022), 13657-13674 Dalton Trans. Dalton Transactions 1477-9226 701699 http://zaguan.unizar.es/record/130600/files/texto_completo.pdf Postprint 2774235 http://zaguan.unizar.es/record/130600/files/texto_completo.jpg?subformat=icon icon Postprint oai:zaguan.unizar.es:130600 articulos driver 2024-03-18-15:26:52 ARTICLE