000078316 001__ 78316
000078316 005__ 20200113145620.0
000078316 0247_ $$2doi$$a10.1016/j.jinorgbio.2018.02.018
000078316 0248_ $$2sideral$$a105291
000078316 037__ $$aART-2018-105291
000078316 041__ $$aeng
000078316 100__ $$ade la Cueva-Alique, I.
000078316 245__ $$aBiological evaluation of water soluble arene Ru(II) enantiomers with amino-oxime ligands
000078316 260__ $$c2018
000078316 5060_ $$aAccess copy available to the general public$$fUnrestricted
000078316 5203_ $$aNew water soluble, enantiopure arene ruthenium compound SRuSN-(1R, 4S)-[(¿6-p-cymene)Ru{¿NH(Bn), ¿NOH}Cl]Cl (Bn = benzyl, 1a') has been synthesized. The novel compound along with that previously described RRuRN-(1S, 4R)-[(¿6-p-cymene)Ru{¿NH(Bn), ¿NOH}Cl]Cl (1a) was evaluated by polarimetry, ultra-violet and circular dichroism spectroscopy. The structure of novel ruthenium derivative 1a' was determined by single crystal X-ray crystallography. Both enantiomers have been tested against several cancer cell lines in vitro: prostate PC-3, lung A-549, pancreas MIA PaCa-2, colorectal HCT-116, leukemia Jurkat and cervical HeLa. Both enantiomers are active and versatile cytotoxic agents, showing IC50 values from 2 to 12 times lower than those found for cisplatin in the different cell lines evaluated. The mechanism of cell death induced by the metal compounds was analyzed in A-549 and Jurkat cell lines. Derivatives 1a and 1a' induced apoptotic cell death of A-549 cells while dose-dependent cell death mechanisms have been found in the Jurkat cell line. Compound-DNA interactions have been investigated by equilibrium dialysis, Fluorescence Resonance Energy Transfer (FRET) melting assays and viscometric titrations, revealing moderate binding affinity of 1a and 1a' towards duplex DNA. Finally, the efficacy of 1a in a preliminary in vivo assay of PC-3 xenografts in nude mice has been evaluated, resulting in a promising inhibition of tumor growth by 45%. Analysis of tumor tissue also showed a significant decrease of levels of crucial molecules in the invasive phenotype of PC-3 cells.
000078316 536__ $$9info:eu-repo/grantAgreement/ES/MICINN/CTQ2014-58270-R
000078316 540__ $$9info:eu-repo/semantics/openAccess$$aby-nc-nd$$uhttp://creativecommons.org/licenses/by-nc-nd/3.0/es/
000078316 590__ $$a3.224$$b2018
000078316 591__ $$aCHEMISTRY, INORGANIC & NUCLEAR$$b11 / 45 = 0.244$$c2018$$dQ1$$eT1
000078316 591__ $$aBIOCHEMISTRY & MOLECULAR BIOLOGY$$b127 / 294 = 0.432$$c2018$$dQ2$$eT2
000078316 592__ $$a0.655$$b2018
000078316 593__ $$aInorganic Chemistry$$c2018$$dQ2
000078316 593__ $$aBiochemistry$$c2018$$dQ2
000078316 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/acceptedVersion
000078316 700__ $$aSierra, S.
000078316 700__ $$aMuñoz-Moreno, L.
000078316 700__ $$aPérez-Redondo, A.
000078316 700__ $$aBajo, A.M.
000078316 700__ $$0(orcid)0000-0002-2315-9079$$aMarzo, I.$$uUniversidad de Zaragoza
000078316 700__ $$aGude, L.
000078316 700__ $$aCuenca, T.
000078316 700__ $$aRoyo, E.
000078316 7102_ $$11002$$2050$$aUniversidad de Zaragoza$$bDpto. Bioq.Biolog.Mol. Celular$$cÁrea Biología Celular
000078316 773__ $$g183 (2018), 32-42$$pJ. inorg. biochem.$$tJOURNAL OF INORGANIC BIOCHEMISTRY$$x0162-0134
000078316 8564_ $$s1178293$$uhttps://zaguan.unizar.es/record/78316/files/texto_completo.pdf$$yPostprint
000078316 8564_ $$s54085$$uhttps://zaguan.unizar.es/record/78316/files/texto_completo.jpg?subformat=icon$$xicon$$yPostprint
000078316 909CO $$ooai:zaguan.unizar.es:78316$$particulos$$pdriver
000078316 951__ $$a2020-01-13-14:55:27
000078316 980__ $$aARTICLE