0000000000610416

AUTHOR

Dina Baier

showing 8 related works from this author

Targeting a Targeted Drug: An Approach Toward Hypoxia-Activatable Tyrosine Kinase Inhibitor Prodrugs

2016

Tyrosine kinase inhibitors (TKIs), which have revolutionized cancer therapy over the past 15 years, are limited in their clinical application due to serious side effects. Therefore, we converted two approved TKIs (sunitinib and erlotinib) into 2-nitroimidazole-based hypoxia-activatable prodrugs. Kinetics studies showed very different stabilities over 24 h; however, fast reductive activation via E. coli nitroreductase could be confirmed for both panels. The anticancer activity and signaling inhibition of the compounds against various human cancer cell lines were evaluated in cell culture. These data, together with molecular docking simulations, revealed distinct differences in the impact of …

medicine.drug_classPharmacology010402 general chemistry01 natural sciencesBiochemistryArticleTyrosine-kinase inhibitor03 medical and health sciencesNitroreductase0302 clinical medicinetyrosine kinase inhibitorsDrug DiscoverymedicinecancerEpidermal growth factor receptorGeneral Pharmacology Toxicology and PharmaceuticsPharmacologybiologyhypoxiaSunitinibChemistryOrganic ChemistryProdrugtargeted therapeutic0104 chemical sciencesSettore CHIM/03 - Chimica Generale E InorganicaCell culture030220 oncology & carcinogenesisbiology.proteinMolecular MedicineErlotinibprodrugTyrosine kinasemedicine.drugChemMedChem
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Ruthenium-arene complexes bearing naphthyl-substituted 1,3-dioxoindan-2-carboxamides ligands for G-quadruplex DNA recognition.

2019

Quadruplex nucleic acids – DNA/RNA secondary structures formed in guanine rich sequences – proved to have key roles in the biology of cancers and, as such, in recent years they emerged as promising targets for small molecules. Many reports demonstrated that metal complexes can effectively stabilize quadruplex structures, promoting telomerase inhibition, downregulation of the expression of cancer-related genes and ultimately cancer cell death. Although extensively explored as anticancer agents, studies on the ability of ruthenium arene complexes to interact with quadruplex nucleic acids are surprisingly almost unknown. Herein, we report on the synthesis and characterization of four novel Ru(…

GuanineStereochemistryCell Survivalchemistry.chemical_elementAntineoplastic Agents010402 general chemistryG-quadruplexLigands01 natural sciencesRutheniumInorganic Chemistrychemistry.chemical_compoundStructure-Activity RelationshipCoordination ComplexesPyridineTumor Cells CulturedHumansRuthenium Quadruplex G-quadruplex G4 DNA Cancer Metal Complexesheterocyclic compoundsCell ProliferationDose-Response Relationship DrugMolecular Structure010405 organic chemistryLigandRNASmall molecule3. Good health0104 chemical sciencesRutheniumG-QuadruplexeschemistrySettore CHIM/03 - Chimica Generale E InorganicaCalixarenesDrug Screening Assays AntitumorDNADalton transactions (Cambridge, England : 2003)
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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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CCDC 1989307: Experimental Crystal Structure Determination

2021

Related Article: Federica Guarra, Alessio Terenzi, Christine Pirker, Rossana Passannante, Dina Baier, Ennio Zangrando, Vanessa G��mez���Vallejo, Tarita Biver, Chiara Gabbiani, Walter Berger, Jordi Llop, Luca Salassa|2020|Angew.Chem.,Int.Ed.|59|17130|doi:10.1002/anie.202008046

Space GroupCrystallographyCrystal SystemCrystal Structure(1-butyl-3-methyl-23-dihydro-1H-imidazol-2-yl)-(chloro)-diiodo-gold(iii)Cell ParametersExperimental 3D Coordinates
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CCDC 1870492: Experimental Crystal Structure Determination

2019

Related Article: Laura A. Hager, Stephan Mokesch, Claudia Kieler, Silvia Alonso-de Castro, Dina Baier, Alexander Roller, Wolfgang Kandioller, Bernhard K. Keppler, Walter Berger, Luca Salassa, Alessio Terenzi|2019|Dalton Trans.|48|12040|doi:10.1039/C9DT02078K

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameters(eta6-p-Cymene)-chloro-((13-dioxo-1H-inden-2(3H)-ylidene)((1-naphthylmethyl)amino)methanolato)-ruthenium(ii)Experimental 3D Coordinates
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CCDC 1989306: Experimental Crystal Structure Determination

2021

Related Article: Federica Guarra, Alessio Terenzi, Christine Pirker, Rossana Passannante, Dina Baier, Ennio Zangrando, Vanessa G��mez���Vallejo, Tarita Biver, Chiara Gabbiani, Walter Berger, Jordi Llop, Luca Salassa|2020|Angew.Chem.,Int.Ed.|59|17130|doi:10.1002/anie.202008046

Space GroupCrystallographyCrystal Systembis(1-butyl-3-methyl-23-dihydro-1H-imidazol-2-ylidene)-(diiodo)-gold(iii) hexafluorophosphateCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1870494: Experimental Crystal Structure Determination

2019

Related Article: Laura A. Hager, Stephan Mokesch, Claudia Kieler, Silvia Alonso-de Castro, Dina Baier, Alexander Roller, Wolfgang Kandioller, Bernhard K. Keppler, Walter Berger, Luca Salassa, Alessio Terenzi|2019|Dalton Trans.|48|12040|doi:10.1039/C9DT02078K

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameters(eta6-p-Cymene)-chloro-((13-dioxo-1H-inden-2(3H)-ylidene)((2-(1-naphthyl)ethyl)amino)methanolato)-ruthenium(ii) hydrateExperimental 3D Coordinates
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CCDC 1870493: Experimental Crystal Structure Determination

2019

Related Article: Laura A. Hager, Stephan Mokesch, Claudia Kieler, Silvia Alonso-de Castro, Dina Baier, Alexander Roller, Wolfgang Kandioller, Bernhard K. Keppler, Walter Berger, Luca Salassa, Alessio Terenzi|2019|Dalton Trans.|48|12040|doi:10.1039/C9DT02078K

Space GroupCrystallographyCrystal System(eta6-p-Cymene)-((13-dioxo-1H-inden-2(3H)-ylidene)((1-naphthylmethyl)amino)methanolato)-pyridine-ruthenium(ii) hexafluorophosphateCrystal StructureCell ParametersExperimental 3D Coordinates
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