000089790 001__ 89790
000089790 005__ 20211117102005.0
000089790 0247_ $$2doi$$a10.1039/c9dt04423j
000089790 0248_ $$2sideral$$a117901
000089790 037__ $$aART-2020-117901
000089790 041__ $$aeng
000089790 100__ $$0(orcid)0000-0002-6674-7364$$aAbas, E.
000089790 245__ $$aNew selective thiolate gold(i) complexes inhibit the proliferation of different human cancer cells and induce apoptosis in primary cultures of mouse colon tumors
000089790 260__ $$c2020
000089790 5060_ $$aAccess copy available to the general public$$fUnrestricted
000089790 5203_ $$aNew thiolate gold(I) complexes with P(NMe2)3 (HMPT) as a phosphane group [Au(SR)(HMPT)] (SR = Spy, Spyrim, SMe2pyrim, Sbenzothiazole, Sthiazoline, Sbenzimidazole and 2-thiouracil) have been synthesized. All of them have been characterized, including X-ray studies of complexes with SMe2pyrim, Sbenzothiazole and 2-thiouracil moieties. In addition, their potential application as anticancer drugs has been analyzed by determining their pharmacokinetic activities (water solubility, cell permeability and BSA transport protein affinity). Based on the good results of these experiments, we carried out the studies of cell viability with our compounds on different cell lines (A2780, A2780R and Caco-2/TC7 cells), showing higher cytotoxic activity than cisplatin in all cases. Besides, two of the synthesized complexes with Sbenzimidazole and 2-thiouracil groups exhibit specific selectivity for cancerous Caco-2 cells and are considered as potential candidates for anticancer drugs. These complexes were able to induce a strong inhibition of the thioredoxin reductase (TrxR) protein and oxidative damage in membrane lipids. Additional studies in primary cultures of mouse colon tumors showed that these two complexes are proapoptotic upon exposure to phosphatidylserine. Based on our results, we conclude that two of our thiolate gold(I) complexes are good and effective candidates for use in chemotherapy.
000089790 536__ $$9info:eu-repo/grantAgreement/ES/DGA-FEDER/A02-17R
000089790 540__ $$9info:eu-repo/semantics/openAccess$$aAll rights reserved$$uhttp://www.europeana.eu/rights/rr-f/
000089790 590__ $$a4.39$$b2020
000089790 591__ $$aCHEMISTRY, INORGANIC & NUCLEAR$$b8 / 45 = 0.178$$c2020$$dQ1$$eT1
000089790 592__ $$a0.98$$b2020
000089790 593__ $$aInorganic Chemistry$$c2020$$dQ1
000089790 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/acceptedVersion
000089790 700__ $$aPena-Martinez, R.
000089790 700__ $$0(orcid)0000-0002-1829-6319$$aAguirre-Ramírez, D.
000089790 700__ $$aRodriguez-Dieguez, A.
000089790 700__ $$0(orcid)0000-0002-5801-3352$$aLaguna, M.
000089790 700__ $$0(orcid)0000-0002-5306-9365$$aGrasa, L.$$uUniversidad de Zaragoza
000089790 7102_ $$11005$$2410$$aUniversidad de Zaragoza$$bDpto. Farmacología y Fisiolog.$$cÁrea Fisiología
000089790 773__ $$g49, 6 (2020), 1915-1927$$pDalton Trans.$$tDalton Transactions$$x1477-9226
000089790 8564_ $$s1004035$$uhttps://zaguan.unizar.es/record/89790/files/texto_completo.pdf$$yPostprint
000089790 8564_ $$s163343$$uhttps://zaguan.unizar.es/record/89790/files/texto_completo.jpg?subformat=icon$$xicon$$yPostprint
000089790 909CO $$ooai:zaguan.unizar.es:89790$$particulos$$pdriver
000089790 951__ $$a2021-11-15-14:35:20
000089790 980__ $$aARTICLE