doi:10.1021/acs.inorgchem.9b02528engAbas, ElisaEspallargas, NataliaBurbello, GianlucaMesonero, José E.Rodriguez-Dieguez, AntonioGrasa, LauraLaguna, MarianoAnticancer Activity of Alkynylgold(I) with P(NMe2)3 Phosphane in Mouse Colon Tumors and Human Colon Carcinoma Caco-2 Cell LineART-2019-115980New 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.2019http://zaguan.unizar.es/record/12999510.1021/acs.inorgchem.9b02528http://zaguan.unizar.es/record/129995oai:zaguan.unizar.es:129995Inorganic Chemistry 58, 22 (2019), 15536-15551All rights reservedhttp://www.europeana.eu/rights/rr-f/info:eu-repo/semantics/openAccess