000129995 001__ 129995
000129995 005__ 20240118092026.0
000129995 0247_ $$2doi$$a10.1021/acs.inorgchem.9b02528
000129995 0248_ $$2sideral$$a115980
000129995 037__ $$aART-2019-115980
000129995 041__ $$aeng
000129995 100__ $$0(orcid)0000-0002-6674-7364$$aAbas, Elisa
000129995 245__ $$aAnticancer Activity of Alkynylgold(I) with P(NMe2)3 Phosphane in Mouse Colon Tumors and Human Colon Carcinoma Caco-2 Cell Line
000129995 260__ $$c2019
000129995 5060_ $$aAccess copy available to the general public$$fUnrestricted
000129995 5203_ $$aNew alkynylgold(I) with P(NMe2)3 (HMPT) phosphane complexes, [Au(CC-R)(HMPT)] (R= 4-Ph, 4-MePh, 4-OMe, 4-Br, 4-Cl, 2-py, and 3-py) have been synthesized and characterized, including X-ray studies of complexes with R= 4-OMe and 4-Br; additionally, their physicochemical properties and anticancer activity have been tested. Due to the great water solubility of the HMPT phosphane, all the complexes exhibit an optimal balance of hydrophilicity/lipophilicity. Also, all of these complexes are quite stable in physiological conditions and interact well enough with the transport protein BSA. All complexes exhibit a higher anticancer activity against Caco-2 cells than cisplatin, and some of them do not present cytotoxic activity against enterocyte-like differentiated cells. The selective complexes are proapoptotic drugs by the exposure of phosphatidylserine, results that are also confirmed in primary cultures from mouse colon tumors. Complexes with a halogen unit also arrest the cell cycle in G2/M phase. It is thought that maybe these apoptosis processes are promoted by the observed oxidative damage in the membrane lipids, as a consequence of the inhibition of the thioredoxin reductase enzyme. Based on our results, we conclude that five of our complexes are good candidates to be used in chemotherapy.
000129995 540__ $$9info:eu-repo/semantics/openAccess$$aAll rights reserved$$uhttp://www.europeana.eu/rights/rr-f/
000129995 590__ $$a4.825$$b2019
000129995 591__ $$aCHEMISTRY, INORGANIC & NUCLEAR$$b4 / 45 = 0.089$$c2019$$dQ1$$eT1
000129995 592__ $$a1.349$$b2019
000129995 593__ $$aChemistry (miscellaneous)$$c2019$$dQ1
000129995 593__ $$aPhysical and Theoretical Chemistry$$c2019$$dQ1
000129995 593__ $$aInorganic Chemistry$$c2019$$dQ1
000129995 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/acceptedVersion
000129995 700__ $$aEspallargas, Natalia
000129995 700__ $$aBurbello, Gianluca
000129995 700__ $$0(orcid)0000-0003-4758-3998$$aMesonero, José E.$$uUniversidad de Zaragoza
000129995 700__ $$aRodriguez-Dieguez, Antonio
000129995 700__ $$0(orcid)0000-0002-5306-9365$$aGrasa, Laura$$uUniversidad de Zaragoza
000129995 700__ $$0(orcid)0000-0002-5801-3352$$aLaguna, Mariano
000129995 7102_ $$11005$$2410$$aUniversidad de Zaragoza$$bDpto. Farmacología y Fisiolog.$$cÁrea Fisiología
000129995 773__ $$g58, 22 (2019), 15536-15551$$pInorg. chem.$$tInorganic Chemistry$$x0020-1669
000129995 8564_ $$s1950499$$uhttps://zaguan.unizar.es/record/129995/files/texto_completo.pdf$$yPostprint
000129995 8564_ $$s929536$$uhttps://zaguan.unizar.es/record/129995/files/texto_completo.jpg?subformat=icon$$xicon$$yPostprint
000129995 909CO $$ooai:zaguan.unizar.es:129995$$particulos$$pdriver
000129995 951__ $$a2024-01-18-09:04:42
000129995 980__ $$aARTICLE