Search results for "metallodrugs"

showing 3 items of 3 documents

Cytotoxic Activity of Organotin(IV) Derivatives with Triazolopyrimidine Containing Exocyclic Oxygen Atoms

2020

In this study cytotoxicity of organotin(IV) compounds with 1,2,4-triazolo[1,5-a]pyrimidines, Me3Sn(5tpO) (1), n-Bu3Sn(5tpO) (2), Me3Sn(mtpO) (3), n-Bu3Sn(mtpO) (4), n-Bu3Sn(HtpO2) (5), Ph3Sn(HtpO2) (6) where 5HtpO = 4,5-dihydro-5-oxo-[1,2,4]triazolo-[1,5-a]pyrimidine, HmtpO = 4,7-dihydro-5-methyl-7-oxo-[1,2,4]triazolo-[1,5-a]pyrimidine, and H2tpO2 = 4,5,6,7-tetrahydro-5,7- dioxo-[1,2,4]triazolo-[1,5-a]-pyrimidine, was assessed on three different human tumor cell lines: HCT-116 (colorectal carcinoma), HepG2 (hepatocarcinoma) and MCF-7 (breast cancer). While 1 and 3 were inactive, compounds 2, 4, 5 and 6 inhibited the growth of the three tumor cell lines with IC50 values in the submicromolar …

DenticityCellPharmaceutical Science01 natural sciencesAnalytical Chemistrychemistry.chemical_compoundDrug DiscoveryOrganotin CompoundstriazolopyrimidineCytotoxicityMembrane Potential MitochondrialCytotoxinsapoptosisBiological activityHep G2 CellsG2 Phase Cell Cycle CheckpointsGene Expression Regulation Neoplasticmedicine.anatomical_structureChemistry (miscellaneous)Mitochondrial MembranesMCF-7 CellsMolecular MedicineCyclin-Dependent Kinase Inhibitor p21crystal structurein vitro anticancer activityPyrimidineCell SurvivalStereochemistryorganotin(iv)010402 general chemistryArticlelcsh:QD241-441Inhibitory Concentration 50Structure-Activity Relationshiplcsh:Organic chemistrymedicineHumansPhysical and Theoretical ChemistryMetallodrug010405 organic chemistryLigandOrganic ChemistryTriazolesHCT116 CellsapoptosiG1 Phase Cell Cycle Checkpoints0104 chemical sciencesPyrimidineschemistrymetallodrugsCell cultureApoptosisDrug DesignTumor Suppressor Protein p53Reactive Oxygen SpeciesMolecules
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Poly(alkylidenimine) Dendrimers Functionalized with the Organometallic Moiety [Ru(η5-C5H5)(PPh3)2]+ as Promising Drugs Against Cisplatin-Resistant Ca…

2018

Here and for the first time, we show that the organometallic compound [Ru(&eta

Pharmaceutical Sciencecisplatin01 natural sciencesAnalytical ChemistrydendrimersCoordination ComplexesDrug DiscoveryMoietyplatinummetallitta116Molecular StructureChemistrymolekyylitnanomedicineNanomedicineChemistry (miscellaneous)MCF-7 CellsMolecular MedicineplatinaDendrimersEpithelial-Mesenchymal TransitionCell SurvivalAntineoplastic Agents.myrkyllisyys010402 general chemistryArticlecancer treatmentlcsh:QD241-441Faculdade de Ciências Exatas e da Engenharialcsh:Organic chemistryDendrimerCell Line TumorOrganometallic CompoundsHumansPhysical and Theoretical ChemistryrutheniumPlatinumCell ProliferationTumor microenvironmentCancer och onkologiToxicitynanocarrierssyöpähoidot010405 organic chemistryOrganic ChemistryMesenchymal stem celltoxicityMesenchymal Stem CellsCombinatorial chemistrykantasolutnanolääketiede0104 chemical scienceslääkkeetTumor progressionCell cultureDrug Resistance NeoplasmmetallodrugsCancer and OncologyCancer cellNanocarriersCaco-2 CellsDrug Screening Assays Antitumor<i>cisplatin</i>hMSCs
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124I Radiolabeling of a AuIII‐NHC Complex for In Vivo Biodistribution Studies†

2020

Abstract AuIII complexes with N‐heterocyclic carbene (NHC) ligands have shown remarkable potential as anticancer agents, yet their fate in vivo has not been thoroughly examined and understood. Reported herein is the synthesis of new AuIII‐NHC complexes by direct oxidation with radioactive [124I]I2 as a valuable strategy to monitor the in vivo biodistribution of this class of compounds using positron emission tomography (PET). While in vitro analyses provide direct evidence for the importance of AuIII‐to‐AuI reduction to achieve full anticancer activity, in vivo studies reveal that a fraction of the AuIII‐NHC prodrug is not immediately reduced after administration but able to reach the major…

Imaging Agents | Hot Paperpositron emission tomography010405 organic chemistryChemistryGeneral ChemistryProdrug010402 general chemistryanticancer01 natural sciencesCombinatorial chemistryCatalysisIn vitro3. Good health0104 chemical sciencesIn vivoIn vivo biodistributionSettore CHIM/03 - Chimica Generale E InorganicametallodrugsN-heterocyclic carbenesanticancer; metallodrugs; N-heterocyclic carbenes; positron emission tomography; radiochemistryradiochemistryResearch ArticlesResearch ArticleAngewandte Chemie (International Ed. in English)
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