Aygün, MuhittinAlper, PınarUlukaya, Engin2024-03-252024-03-252018-07-24İcsel, C. vd. (2018). ''Palladium(II) and platinum(II ) saccharinate complexes with bis(diphenylphosphino)methane/ ethane: synthesis, S-phase arrest and ROS- mediated apoptosis in human colon cancer cells''. Dalton Transactions, 47(33), 11397-11410.1477-9226https://pubs.rsc.org/en/content/articlelanding/2018/dt/c8dt02389ahttps://hdl.handle.net/11452/40609New neutral [M(sac)(2)(diphos)] and cationic [M(diphos)(2)](sac)(2) complexes, where M = Pd-II or Pt-II, sac = saccharinate, and diphos = 1,1-bis(diphenylphosphino)methane (dppm) or 1,2-bis(diphenylphosphino)ethane (dppe), were synthesized and structurally characterized. The anticancer activity of the complexes was investigated against MCF-7 (breast), A549 (lung), HCT116 (colon), DU145 (prostate) cancer and BEAS-2B (normal bronchial epithelial) cells. Neutral Pt-dppm (2) and Pd-dppe complexes (5) did not show any biological activity. The cationic Pd-dppe (7) complex displayed antiproliferative activity, while the rest of the complexes exhibited potent cytotoxicity compared with cisplatin. The active Pd(ii)/Pt(ii) complexes were then included in further studies including interaction with DNA/HSA, nuclease activity, cellular uptake and lipophilicity. The potent complexes induced the apoptotic cell death as probed through annexin V positivity and caspase activation. Mechanistic studies on HCT116 cells showed that the complexes cause cell cycle arrest at the DNA synthesis (S) phase and excessive generation of reactive oxygen species (ROS), damaging to both mitochondria and DNA.eninfo:eu-repo/semantics/closedAccessAdsorptive stripping voltammetryThiosaccharinate tsac complexesAscites-carcinoma eacDNA-binding agentsIn-vitroCrystal-structuresAntiproliferative activityMolecular-mechanismsAnticancer activityThermal-propertiesBioactivityCell deathCytotoxicityDiseasesDNAMethanePlatinum compoundsSynthesis (chemical)Anti-proliferative activitiesAnticancer activitiesApoptotic cell deathCaspase activationHuman colon cancer cellsInteraction with dnasMechanistic studiesReactive oxygen speciesPalladium compoundsChemistryAntineoplastic agentsApoptosisBiological transportChemistry techniques, syntheticColonic neoplasmsDNADNA breaks, double-strandedEthaneHCT116 cellsHumansHydrophobic and hydrophilic interactionsMembrane potential, mitochondrialMethaneMolecular docking simulationNucleic acid conformationOrganoplatinum compoundsPalladiumPlatinumProtein conformationReactive oxygen speciesS phase cell cycle checkpointsSerum albumin, humanArticle0004425097000142-s2.0-850520003631139711410473330062356https://doi.org/10.1039/c8dt02389aChemistry, inorganic & nuclearComplex; Palladium; 2-PhenylpyridineAntineoplastic agentDNAEthaneHuman serum albuminMethanePalladiumPlatinumPlatinum complexReactive oxygen metaboliteApoptosisChemical phenomenaChemistryColon tumorConformationDouble stranded DNA breakDrug effectHCT 116 cell lineHumanMetabolismMitochondrial membrane potentialMolecular dockingPathologyProtein conformationS phase cell cycle checkpointSynthesisTransport at the cellular level1477-9234