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  1. Article ; Online: In vitro biodistribution studies on clinically approved FGFR inhibitors ponatinib, nintedanib, erlotinib and the investigational inhibitor KP2692.

    Dömötör, Orsolya / Mathuber, Marlene / Kowol, Christian R

    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

    2023  Volume 192, Page(s) 106651

    Abstract: Binding towards human serum albumin (HSA) and α1-acid glycoprotein (AGP) of three approved fibroblast growth factor receptor (FGFR) inhibitors ponatinib (PON), nintedanib (NIN) and erdafitinib (ERD), as well as the experimental drug KP2692 was studied by ...

    Abstract Binding towards human serum albumin (HSA) and α1-acid glycoprotein (AGP) of three approved fibroblast growth factor receptor (FGFR) inhibitors ponatinib (PON), nintedanib (NIN) and erdafitinib (ERD), as well as the experimental drug KP2692 was studied by means of spectrofluorometric and UV-visible spectrophotometric methods. Additionally, proton dissociation processes, lipophilicity, and fluorescence properties of these four molecules were investigated in detail. The FGFR inhibitors were predominantly presented in their single protonated form (HL
    MeSH term(s) Humans ; Erlotinib Hydrochloride/pharmacology ; Tissue Distribution ; Imidazoles/pharmacology ; Serum Albumin, Human ; Protein Binding
    Chemical Substances Erlotinib Hydrochloride (DA87705X9K) ; ponatinib (4340891KFS) ; nintedanib (G6HRD2P839) ; Imidazoles ; Serum Albumin, Human (ZIF514RVZR)
    Language English
    Publishing date 2023-11-25
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1154366-8
    ISSN 1879-0720 ; 0928-0987
    ISSN (online) 1879-0720
    ISSN 0928-0987
    DOI 10.1016/j.ejps.2023.106651
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  2. Article: Einbau von (Bioaktiven) Äquatorialen Liganden in Platin(IV)-Komplexe.

    Kastner, Alexander / Schueffl, Hemma / Yassemipour, Patrick A / Keppler, Bernhard K / Heffeter, Petra / Kowol, Christian R

    Angewandte Chemie (Weinheim an der Bergstrasse, Germany)

    2023  Volume 135, Issue 46, Page(s) e202311468

    Language English
    Publishing date 2023-10-13
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 506609-8
    ISSN 1521-3757 ; 0044-8249 ; 0932-2140
    ISSN (online) 1521-3757
    ISSN 0044-8249 ; 0932-2140
    DOI 10.1002/ange.202311468
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  3. Article ; Online: Insertion of (Bioactive) Equatorial Ligands into Platinum(IV) Complexes.

    Kastner, Alexander / Schueffl, Hemma / Yassemipour, Patrick A / Keppler, Bernhard K / Heffeter, Petra / Kowol, Christian R

    Angewandte Chemie (International ed. in English)

    2023  Volume 62, Issue 46, Page(s) e202311468

    Abstract: Platinum(IV) prodrugs are highly interesting alternatives to platinum(II) anticancer therapeutics due to their increased tumor selectivity and reduced side effects. In contrast to the established theory, we recently observed that the equatorial ligand(s) ...

    Abstract Platinum(IV) prodrugs are highly interesting alternatives to platinum(II) anticancer therapeutics due to their increased tumor selectivity and reduced side effects. In contrast to the established theory, we recently observed that the equatorial ligand(s) of e.g. oxaliplatin(IV) complexes can be hydrolyzed with formation of [(DACH)Pt(OH
    MeSH term(s) Humans ; Platinum ; Oxaliplatin ; Organoplatinum Compounds ; Ligands ; Prodrugs ; Neoplasms ; Antineoplastic Agents ; Cell Line, Tumor
    Chemical Substances Platinum (49DFR088MY) ; Oxaliplatin (04ZR38536J) ; Organoplatinum Compounds ; Ligands ; Prodrugs ; Antineoplastic Agents
    Language English
    Publishing date 2023-10-13
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.202311468
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  4. Article: Tumor-targeted dual-action NSAID-platinum(iv) anticancer prodrugs.

    Kastner, Alexander / Mendrina, Theresa / Bachmann, Florian / Berger, Walter / Keppler, Bernhard K / Heffeter, Petra / Kowol, Christian R

    Inorganic chemistry frontiers

    2023  Volume 10, Issue 14, Page(s) 4126–4138

    Abstract: Platinum(iv) prodrugs are a promising class of anticancer agents designed to overcome the limitations of conventional platinum(ii) therapeutics. In this work, we present oxaliplatin(iv)-based complexes, which upon reduction, release acetylsalicylic acid ( ...

    Abstract Platinum(iv) prodrugs are a promising class of anticancer agents designed to overcome the limitations of conventional platinum(ii) therapeutics. In this work, we present oxaliplatin(iv)-based complexes, which upon reduction, release acetylsalicylic acid (aspirin), known for its antitumor activity against colon cancer and currently investigated in combination with oxaliplatin in a phase III clinical study. Comparison with a recently reported cisplatin analog (asplatin) revealed a massive increase in reduction stability for the oxaliplatin complex in mouse serum. This was in line with the cell culture data indicating the desired prodrug properties for the newly synthesized complex. For
    Language English
    Publishing date 2023-06-28
    Publishing country England
    Document type Journal Article
    ISSN 2052-1553
    ISSN 2052-1553
    DOI 10.1039/d3qi00968h
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  5. Article ; Online: A Comparative Study on the Complexation of the Anticancer Iron Chelator VLX600 with Essential Metal Ions.

    Pósa, Vivien / Federa, Anja / Cseh, Klaudia / Wenisch, Dominik / Spengler, Gabriella / May, Nóra V / Lihi, Norbert / Samu, Gergely F / Jakupec, Michael A / Keppler, Bernhard K / Kowol, Christian R / Enyedy, Éva A

    Inorganic chemistry

    2024  Volume 63, Issue 5, Page(s) 2401–2417

    Abstract: As cancer cells exhibit an increased uptake of iron, targeting the interaction with iron has become a straightforward strategy in the fight against cancer. This work comprehensively characterizes the chemical properties of 6-methyl-3-{( ... ...

    Abstract As cancer cells exhibit an increased uptake of iron, targeting the interaction with iron has become a straightforward strategy in the fight against cancer. This work comprehensively characterizes the chemical properties of 6-methyl-3-{(2
    MeSH term(s) Humans ; Ferric Compounds ; Copper/pharmacology ; Copper/chemistry ; Metals/chemistry ; Iron/chemistry ; Ions ; Coordination Complexes/pharmacology ; Coordination Complexes/chemistry ; Iron Chelating Agents/pharmacology ; Ferrous Compounds ; Hydrazones ; Triazoles
    Chemical Substances VLX600 ; Ferric Compounds ; Copper (789U1901C5) ; Metals ; Iron (E1UOL152H7) ; Ions ; Coordination Complexes ; Iron Chelating Agents ; Ferrous Compounds ; Hydrazones ; Triazoles
    Language English
    Publishing date 2024-01-24
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1484438-2
    ISSN 1520-510X ; 0020-1669
    ISSN (online) 1520-510X
    ISSN 0020-1669
    DOI 10.1021/acs.inorgchem.3c03259
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  6. Article ; Online: Schiff bases and their metal complexes to target and overcome (multidrug) resistance in cancer.

    Podolski-Renić, Ana / Čipak Gašparović, Ana / Valente, Andreia / López, Óscar / Bormio Nunes, Julia H / Kowol, Christian R / Heffeter, Petra / Filipović, Nenad R

    European journal of medicinal chemistry

    2024  Volume 270, Page(s) 116363

    Abstract: Overcoming multidrug resistance (MDR) is one of the major challenges in cancer therapy. In this respect, Schiff base-related compounds (bearing a ... ...

    Abstract Overcoming multidrug resistance (MDR) is one of the major challenges in cancer therapy. In this respect, Schiff base-related compounds (bearing a R
    MeSH term(s) Coordination Complexes/pharmacology ; Coordination Complexes/chemistry ; Schiff Bases/pharmacology ; Schiff Bases/chemistry ; Drug Resistance, Multiple ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/chemistry ; Neoplasms/drug therapy
    Chemical Substances Coordination Complexes ; Schiff Bases ; Antineoplastic Agents
    Language English
    Publishing date 2024-03-29
    Publishing country France
    Document type Journal Article ; Review
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2024.116363
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  7. Article ; Online: Liposomal formulations of anticancer copper(II) thiosemicarbazone complexes.

    Mathuber, Marlene / Hager, Sonja / Keppler, Bernhard K / Heffeter, Petra / Kowol, Christian R

    Dalton transactions (Cambridge, England : 2003)

    2021  Volume 50, Issue 44, Page(s) 16053–16066

    Abstract: α-N-Heterocyclic thiosemicarbazones such as triapine and COTI-2 are currently investigated as anticancer therapeutics in clinical trials. However, triapine was widely inactive against solid tumor types. A likely explanation is the short plasma half-life ... ...

    Abstract α-N-Heterocyclic thiosemicarbazones such as triapine and COTI-2 are currently investigated as anticancer therapeutics in clinical trials. However, triapine was widely inactive against solid tumor types. A likely explanation is the short plasma half-life time and fast metabolism. One promising approach to overcome these drawbacks is the encapsulation of the drug into nanoparticles (passive drug-targeting). In a previous work we showed that it was not possible to stably encapsulate free triapine into liposomes. Hence, in this manuscript we present the successful preparation of liposomal formulations of the copper(II) complexes of triapine and COTI-2. To this end, various drug-loading strategies were examined and the resulting liposomes were physico-chemically characterized. Especially for liposomal Cu-triapine, a decent encapsulation efficacy and a slow drug release behavior could be observed. In contrast, for COTI-2 and its copper(II) complex no stable loading could be achieved. Subsequent
    MeSH term(s) Animals ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacokinetics ; Cell Line, Tumor ; Cell Survival/drug effects ; Coordination Complexes/administration & dosage ; Coordination Complexes/chemistry ; Coordination Complexes/pharmacokinetics ; Copper/administration & dosage ; Copper/chemistry ; Copper/pharmacokinetics ; Drug Liberation ; Female ; Humans ; Liposomes ; Methemoglobin/metabolism ; Mice, Inbred BALB C ; Thiosemicarbazones/administration & dosage ; Thiosemicarbazones/chemistry ; Thiosemicarbazones/pharmacokinetics ; Mice
    Chemical Substances Antineoplastic Agents ; Coordination Complexes ; Liposomes ; Thiosemicarbazones ; Copper (789U1901C5) ; Methemoglobin (9008-37-1)
    Language English
    Publishing date 2021-11-16
    Publishing country England
    Document type Journal Article
    ZDB-ID 1472887-4
    ISSN 1477-9234 ; 1364-5447 ; 0300-9246 ; 1477-9226
    ISSN (online) 1477-9234 ; 1364-5447
    ISSN 0300-9246 ; 1477-9226
    DOI 10.1039/d1dt02763h
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  8. Article ; Online: Novel oxaliplatin(IV) complexes conjugated with ligands bearing pendant 1,2-dithiolane/1,2-diselenolane/cyclopentyl motifs.

    Liu, Xiao / Wenisch, Dominik / Barth, Marie-Christin / Cseh, Klaudia / Kowol, Christian R / Jakupec, Michael A / Gibson, Dan / Keppler, Bernhard K / Weigand, Wolfgang

    Dalton transactions (Cambridge, England : 2003)

    2022  Volume 51, Issue 44, Page(s) 16824–16835

    Abstract: In this work, biologically active α-lipoic acid (ALA) and its isologous 1,2-diselenolane (SeA) and cyclopentyl (CpA) analogues were investigated for their differences in redox potentials, cytotoxicity and ROS production. In addition, the corresponding Pt( ...

    Abstract In this work, biologically active α-lipoic acid (ALA) and its isologous 1,2-diselenolane (SeA) and cyclopentyl (CpA) analogues were investigated for their differences in redox potentials, cytotoxicity and ROS production. In addition, the corresponding Pt(IV) complexes comprising ALA (1-4), SeA (5-8) and CpA (9-12) as axial ligands were synthesized. Those Pt(IV) complexes were characterized by NMR spectroscopy, ESI-mass spectrometry and elemental analysis. The cytotoxicity study showed that 1,2-diselenolane containing Pt(IV) (1, 3 and 4) complexes are more cytotoxic than the 1,2-dithiolane analogues (5, 7, and 8) throughout all tested cell lines, intriguingly, cyclopentyl containing species (9, 11 and 12) are the most effective, in some cases even more potent than the parent drug oxaliplatin. Three representative complexes 2, 6 and 10 were further assessed for their redox potentials, reduction with AsA, lipophilicity, cellular accumulation and ROS production. It turned out that the cytotoxicity profile is an overall result of good lipophilicity, high cellular accumulation, and (partially) enhanced ROS generation.
    MeSH term(s) Oxaliplatin/pharmacology ; Ligands ; Reactive Oxygen Species/metabolism ; Cell Line, Tumor ; Antineoplastic Agents/chemistry
    Chemical Substances Oxaliplatin (04ZR38536J) ; Ligands ; Reactive Oxygen Species ; 1,2-dithiolane ; Antineoplastic Agents
    Language English
    Publishing date 2022-11-15
    Publishing country England
    Document type Journal Article
    ZDB-ID 1472887-4
    ISSN 1477-9234 ; 1364-5447 ; 0300-9246 ; 1477-9226
    ISSN (online) 1477-9234 ; 1364-5447
    ISSN 0300-9246 ; 1477-9226
    DOI 10.1039/d2dt02217f
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  9. Article ; Online: The coordination modes of (thio)semicarbazone copper(II) complexes strongly modulate the solution chemical properties and mechanism of anticancer activity.

    Pósa, Vivien / Hajdu, Bálint / Tóth, Gábor / Dömötör, Orsolya / Kowol, Christian R / Keppler, Bernhard K / Spengler, Gabriella / Gyurcsik, Béla / Enyedy, Éva A

    Journal of inorganic biochemistry

    2022  Volume 231, Page(s) 111786

    Abstract: Thiosemicarbazones are promising candidates for anticancer therapy and their mechanism of action is often linked to their metal chelating ability. In this study, five (thio)semicarbazones with different donor sets (NNS, NNO, ONS, ONO) were selected and ... ...

    Abstract Thiosemicarbazones are promising candidates for anticancer therapy and their mechanism of action is often linked to their metal chelating ability. In this study, five (thio)semicarbazones with different donor sets (NNS, NNO, ONS, ONO) were selected and their behaviour in aqueous solution, the stability of their copper(II) complexes in addition to their cytotoxicity, DNA-binding, DNA cleavage ability and inhibition of topoisomerase IIα were investigated and compared. We aimed to reveal relationships between the structural variations, the significantly different physico-chemical properties, solution speciation and biological activity. The cytotoxicity of the ligands did not show correlation with the solubility, lipophilicity and permeability; and the decreased activity of the oxygen donor containing compounds was explained by their stronger preference towards chelation of iron(III) over iron(II). Meanwhile, among the copper complexes the most lipophilic species with the highest stability and membrane permeability exhibited the highest cytotoxicity. The studied copper(II) complexes interact with DNA, and reaction with glutathione led to heavy DNA cleavage in the case of the highly stable complexes which could be reduced in a reversible reaction with moderate rate. All the tested copper complexes inhibited topoisomerase IIα, however, this property of the complexes with low stability is most probably linked to the liberated free copper(II).
    MeSH term(s) Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Coordination Complexes/chemistry ; Coordination Complexes/pharmacology ; Copper/chemistry ; Ferric Compounds ; Semicarbazones/pharmacology
    Chemical Substances Antineoplastic Agents ; Coordination Complexes ; Ferric Compounds ; Semicarbazones ; Copper (789U1901C5)
    Language English
    Publishing date 2022-03-06
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 162843-4
    ISSN 1873-3344 ; 0162-0134
    ISSN (online) 1873-3344
    ISSN 0162-0134
    DOI 10.1016/j.jinorgbio.2022.111786
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    Zs.B 1730: Show issues Location:
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  10. Article ; Online: Oxoplatin-Based Pt(IV) Lipoate Complexes and Their Biological Activity.

    Liu, Xiao / Barth, Marie-Christin / Cseh, Klaudia / Kowol, Christian R / Jakupec, Michael A / Keppler, Bernhard K / Gibson, Dan / Weigand, Wolfgang

    Chemistry & biodiversity

    2022  Volume 19, Issue 10, Page(s) e202200695

    Abstract: α-Lipoic acid, known for its anti-inflammatory and antioxidant activity, represents a promising ligand for Pt(IV) prodrugs. Three new Pt(IV) lipoate complexes were synthesized and characterized by NMR spectroscopy ( ...

    Abstract α-Lipoic acid, known for its anti-inflammatory and antioxidant activity, represents a promising ligand for Pt(IV) prodrugs. Three new Pt(IV) lipoate complexes were synthesized and characterized by NMR spectroscopy (
    MeSH term(s) Antineoplastic Agents/chemistry ; Antioxidants ; Ascorbic Acid ; Cell Line, Tumor ; DNA ; Ligands ; Molecular Structure ; Prodrugs/pharmacology ; Prodrugs/chemistry ; Reactive Oxygen Species/metabolism ; Thioctic Acid
    Chemical Substances Antineoplastic Agents ; Antioxidants ; Ascorbic Acid (PQ6CK8PD0R) ; diamminedichlorodihydroxyplatinum IV (VVI1VF51WL) ; DNA (9007-49-2) ; Ligands ; Prodrugs ; Reactive Oxygen Species ; Thioctic Acid (73Y7P0K73Y) ; 9-methylguanine (397W61ZHWY)
    Language English
    Publishing date 2022-09-20
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2139001-0
    ISSN 1612-1880 ; 1612-1872
    ISSN (online) 1612-1880
    ISSN 1612-1872
    DOI 10.1002/cbdv.202200695
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