000130600 001__ 130600
000130600 005__ 20240319081014.0
000130600 0247_ $$2doi$$a10.1039/d2dt01963a
000130600 0248_ $$2sideral$$a130215
000130600 037__ $$aART-2022-130215
000130600 041__ $$aeng
000130600 100__ $$aGascón, Elena
000130600 245__ $$aGold(I) metallocyclophosphazenes with antibacterial potency and antitumor efficacy. Synergistic antibacterial action of a heterometallic gold and silver-cyclophosphazene
000130600 260__ $$c2022
000130600 5060_ $$aAccess copy available to the general public$$fUnrestricted
000130600 5203_ $$aOne 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.
000130600 536__ $$9info:eu-repo/grantAgreement/ES/DGA/B25-20R$$9info:eu-repo/grantAgreement/ES/DGA/E47-20R$$9info:eu-repo/grantAgreement/ES/DGA-FEDER/Construyendo Europa desde Aragón$$9info:eu-repo/grantAgreement/ES/MINECO/MAT2017-84838-P
000130600 540__ $$9info:eu-repo/semantics/openAccess$$aAll rights reserved$$uhttp://www.europeana.eu/rights/rr-f/
000130600 590__ $$a4.0$$b2022
000130600 591__ $$aCHEMISTRY, INORGANIC & NUCLEAR$$b7 / 42 = 0.167$$c2022$$dQ1$$eT1
000130600 592__ $$a0.79$$b2022
000130600 593__ $$aInorganic Chemistry$$c2022$$dQ1
000130600 594__ $$a7.1$$b2022
000130600 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/acceptedVersion
000130600 700__ $$0(orcid)0000-0003-1027-7583$$aOtal, Isabel$$uUniversidad de Zaragoza
000130600 700__ $$aMaisanaba, Sara
000130600 700__ $$aLlana-Ruiz-Cabello, María
000130600 700__ $$aValero, Eva
000130600 700__ $$aRepetto, Guillermo
000130600 700__ $$aJones, Peter G.
000130600 700__ $$0(orcid)0000-0002-0922-5615$$aOriol, Luis$$uUniversidad de Zaragoza
000130600 700__ $$0(orcid)0000-0002-3444-0851$$aJiménez, Josefina$$uUniversidad de Zaragoza
000130600 7102_ $$12010$$2760$$aUniversidad de Zaragoza$$bDpto. Química Inorgánica$$cÁrea Química Inorgánica
000130600 7102_ $$11011$$2630$$aUniversidad de Zaragoza$$bDpto. Microb.Ped.Radio.Sal.Pú.$$cÁrea Microbiología
000130600 7102_ $$12013$$2765$$aUniversidad de Zaragoza$$bDpto. Química Orgánica$$cÁrea Química Orgánica
000130600 773__ $$g51, 36 (2022), 13657-13674$$pDalton Trans.$$tDalton Transactions$$x1477-9226
000130600 8564_ $$s701699$$uhttps://zaguan.unizar.es/record/130600/files/texto_completo.pdf$$yPostprint
000130600 8564_ $$s2774235$$uhttps://zaguan.unizar.es/record/130600/files/texto_completo.jpg?subformat=icon$$xicon$$yPostprint
000130600 909CO $$ooai:zaguan.unizar.es:130600$$particulos$$pdriver
000130600 951__ $$a2024-03-18-15:26:52
000130600 980__ $$aARTICLE