129995 20240118092026.0 doi 10.1021/acs.inorgchem.9b02528 sideral 115980 ART-2019-115980 eng Abas, Elisa (orcid)0000-0002-6674-7364 Anticancer Activity of Alkynylgold(I) with P(NMe2)3 Phosphane in Mouse Colon Tumors and Human Colon Carcinoma Caco-2 Cell Line 2019 New 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. Access copy available to the general public Unrestricted info:eu-repo/semantics/openAccess All rights reserved http://www.europeana.eu/rights/rr-f/ 4.825 2019 CHEMISTRY, INORGANIC & NUCLEAR 4 / 45 = 0.089 2019 Q1 T1 1.349 2019 Chemistry (miscellaneous) 2019 Q1 Physical and Theoretical Chemistry 2019 Q1 Inorganic Chemistry 2019 Q1 info:eu-repo/semantics/article info:eu-repo/semantics/acceptedVersion Espallargas, Natalia Burbello, Gianluca Mesonero, José E. Universidad de Zaragoza (orcid)0000-0003-4758-3998 Rodriguez-Dieguez, Antonio Grasa, Laura Universidad de Zaragoza (orcid)0000-0002-5306-9365 Laguna, Mariano (orcid)0000-0002-5801-3352 1005 410 Universidad de Zaragoza Dpto. Farmacología y Fisiolog. Área Fisiología 58, 22 (2019), 15536-15551 Inorg. chem. Inorganic Chemistry 0020-1669 1950499 http://zaguan.unizar.es/record/129995/files/texto_completo.pdf Postprint 929536 http://zaguan.unizar.es/record/129995/files/texto_completo.jpg?subformat=icon icon Postprint oai:zaguan.unizar.es:129995 articulos driver 2024-01-18-09:04:42 ARTICLE