89790 20211117102005.0 doi 10.1039/c9dt04423j sideral 117901 ART-2020-117901 eng Abas, E. (orcid)0000-0002-6674-7364 New selective thiolate gold(i) complexes inhibit the proliferation of different human cancer cells and induce apoptosis in primary cultures of mouse colon tumors 2020 Access copy available to the general public Unrestricted New thiolate gold(I) complexes with P(NMe2)3 (HMPT) as a phosphane group [Au(SR)(HMPT)] (SR = Spy, Spyrim, SMe2pyrim, Sbenzothiazole, Sthiazoline, Sbenzimidazole and 2-thiouracil) have been synthesized. All of them have been characterized, including X-ray studies of complexes with SMe2pyrim, Sbenzothiazole and 2-thiouracil moieties. In addition, their potential application as anticancer drugs has been analyzed by determining their pharmacokinetic activities (water solubility, cell permeability and BSA transport protein affinity). Based on the good results of these experiments, we carried out the studies of cell viability with our compounds on different cell lines (A2780, A2780R and Caco-2/TC7 cells), showing higher cytotoxic activity than cisplatin in all cases. Besides, two of the synthesized complexes with Sbenzimidazole and 2-thiouracil groups exhibit specific selectivity for cancerous Caco-2 cells and are considered as potential candidates for anticancer drugs. These complexes were able to induce a strong inhibition of the thioredoxin reductase (TrxR) protein and oxidative damage in membrane lipids. Additional studies in primary cultures of mouse colon tumors showed that these two complexes are proapoptotic upon exposure to phosphatidylserine. Based on our results, we conclude that two of our thiolate gold(I) complexes are good and effective candidates for use in chemotherapy. info:eu-repo/grantAgreement/ES/DGA-FEDER/A02-17R info:eu-repo/semantics/openAccess All rights reserved http://www.europeana.eu/rights/rr-f/ 4.39 2020 CHEMISTRY, INORGANIC & NUCLEAR 8 / 45 = 0.178 2020 Q1 T1 0.98 2020 Inorganic Chemistry 2020 Q1 info:eu-repo/semantics/article info:eu-repo/semantics/acceptedVersion Pena-Martinez, R. Aguirre-Ramírez, D. (orcid)0000-0002-1829-6319 Rodriguez-Dieguez, A. Laguna, M. (orcid)0000-0002-5801-3352 Grasa, L. Universidad de Zaragoza (orcid)0000-0002-5306-9365 1005 410 Universidad de Zaragoza Dpto. Farmacología y Fisiolog. Área Fisiología 49, 6 (2020), 1915-1927 Dalton Trans. Dalton Transactions 1477-9226 1004035 http://zaguan.unizar.es/record/89790/files/texto_completo.pdf Postprint 163343 http://zaguan.unizar.es/record/89790/files/texto_completo.jpg?subformat=icon icon Postprint oai:zaguan.unizar.es:89790 articulos driver 2021-11-15-14:35:20 ARTICLE