@article{MTMT:34761990, title = {Complex formation of ML324, the histone demethylase inhibitor, with essential metal ions: Relationship between solution chemistry and anticancer activity}, url = {https://m2.mtmt.hu/api/publication/34761990}, author = {Kovács, Hilda and Jakusch, Tamás and May, Nóra Veronika and Tóth, Szilárd and Szakács, Gergely and Enyedy, Éva Anna}, doi = {10.1016/j.jinorgbio.2024.112540}, journal-iso = {J INORG BIOCHEM}, journal = {JOURNAL OF INORGANIC BIOCHEMISTRY}, volume = {255}, unique-id = {34761990}, issn = {0162-0134}, year = {2024}, eissn = {1873-3344}, orcid-numbers = {Jakusch, Tamás/0000-0003-0532-5202; May, Nóra Veronika/0000-0003-4770-4681; Enyedy, Éva Anna/0000-0002-8058-8128} } @article{MTMT:33647485, title = {Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency}, url = {https://m2.mtmt.hu/api/publication/33647485}, author = {Orgován, Zoltán and Péczka, Nikolett and Petri, László and Ábrányi-Balogh, Péter and Randelovic, Ivan and Tóth, Szilárd and Szakács, Gergely and Nyíri, Kinga and Vértessy, Beáta (Grolmuszné) and Pálfy, Gyula and Vida, István and Perczel, András and Tóvári, József and Keserű, György Miklós}, doi = {10.1016/j.ejmech.2023.115212}, journal-iso = {EUR J MED CHEM}, journal = {EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY}, volume = {250}, unique-id = {33647485}, issn = {0223-5234}, abstract = {G12C mutant KRas is considered druggable by allele-specific covalent inhibitors due to the nucleophilic character of the oncogenic mutant cysteine at position 12. Discovery of these inhibitors requires the optimization of both covalent and noncovalent interactions. Here, we report covalent fragment screening of our electrophilic fragment library of diverse non-covalent scaffolds equipped with 40 different electrophilic functionalities to identify fragments as suitable starting points targeting Cys12. Screening the library against KRasG12C using Ellman's free thiol assay, followed by protein NMR and cell viability assays, resulted in two potential inhibitor chemotypes. Characterization of these scaffolds in in vitro cellular- and in vivo xenograft models revealed them as promising starting points for covalent drug discovery programs.}, year = {2023}, eissn = {1768-3254}, orcid-numbers = {Randelovic, Ivan/0000-0003-0161-0022; Pálfy, Gyula/0000-0003-1590-5331; Perczel, András/0000-0003-1252-6416; Tóvári, József/0000-0002-5543-3204} } @article{MTMT:33532438, title = {Metal Complexes of a 5-Nitro-8-Hydroxyquinoline-Proline Hybrid with Enhanced Water Solubility Targeting Multidrug Resistant Cancer Cells}, url = {https://m2.mtmt.hu/api/publication/33532438}, author = {Pivarcsik, Tamás and Pósa, Vivien and Kovács, Hilda and May, Nóra Veronika and Spengler, Gabriella and Pósa, Szonja P. and Tóth, Szilárd and Nezafat Yazdi, Zeinab and Laczka, Csilla and Ugrai, Imre and Szatmári, István and Szakács, Gergely and Enyedy, Éva Anna}, doi = {10.3390/ijms24010593}, journal-iso = {INT J MOL SCI}, journal = {INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES}, volume = {24}, unique-id = {33532438}, issn = {1661-6596}, abstract = {Multidrug resistance (MDR) in cancer is one of the major obstacles of chemotherapy. We have recently identified a series of 8-hydroxyquinoline Mannich base derivatives with MDR-selective toxicity, however with limited solubility. In this work, a novel 5-nitro-8-hydroxyquinoline-proline hybrid and its Rh(η5-C5Me5) and Ru(η6-p-cymene) complexes with excellent aqueous solubility were developed, characterized, and tested against sensitive and MDR cells. Complex formation of the ligand with essential metal ions was also investigated using UV-visible, circular dichroism, 1H NMR (Zn(II)), and electron paramagnetic resonance (Cu(II)) spectroscopic methods. Formation of mono and bis complexes was found in all cases with versatile coordination modes, while tris complexes were also formed with Fe(II) and Fe(III) ions, revealing the metal binding affinity of the ligand at pH 7.4: Cu(II) > Zn(II) > Fe(II) > Fe(III). The ligand and its Rh(III) complex displayed enhanced cytotoxicity against the resistant MES-SA/Dx5 and Colo320 human cancer cell lines compared to their chemosensitive counterparts. Both organometallic complexes possess high stability in solution, however the Ru(II) complex has lower chloride ion affinity and slower ligand exchange processes, along with the readiness to lose the arene ring that is likely connected to its inactivity.}, year = {2023}, eissn = {1422-0067}, orcid-numbers = {May, Nóra Veronika/0000-0003-4770-4681; Spengler, Gabriella/0000-0001-8085-0950; Pósa, Szonja P./0000-0002-7535-9689; Szatmári, István/0000-0002-8571-5229; Enyedy, Éva Anna/0000-0002-8058-8128} } @article{MTMT:33083436, title = {Optimized Synthesis and Cytotoxic Activity of α Aminophosphonates against a Multidrug Resistant Uterine Sarcoma Cell Line}, url = {https://m2.mtmt.hu/api/publication/33083436}, author = {Varga, Petra Regina and Dinnyési, Emőke and Tóth, Szilárd and Szakács, Gergely and Keglevich, György}, doi = {10.2174/1570180819666220609104427}, journal-iso = {LETT DRUG DES DISCOV}, journal = {LETTERS IN DRUG DESIGN AND DISCOVERY}, volume = {20}, unique-id = {33083436}, issn = {1570-1808}, year = {2023}, eissn = {1875-628X}, pages = {365-371} } @article{MTMT:32848262, title = {Cytotoxicity of cinchona alkaloid organocatalysts against MES-SA and MES-SA/Dx5 multidrug-resistant uterine sarcoma cell lines}, url = {https://m2.mtmt.hu/api/publication/32848262}, author = {Pósa, Szonja Polett and Dargó, Gyula and Nagy, Sándor and Kisszékelyi, Péter and Garádi, Zsófia and Hámori, Lilla and Szakács, Gergely and Kupai, József and Tóth, Szilárd}, doi = {10.1016/j.bmc.2022.116855}, journal-iso = {BIOORGAN MED CHEM}, journal = {BIOORGANIC & MEDICINAL CHEMISTRY}, volume = {67}, unique-id = {32848262}, issn = {0968-0896}, year = {2022}, eissn = {1464-3391}, orcid-numbers = {Kisszékelyi, Péter/0000-0002-9529-0674; Garádi, Zsófia/0000-0002-0152-2746; Hámori, Lilla/0000-0002-8962-0040; Kupai, József/0000-0002-4212-4517} } @article{MTMT:32843044, title = {Structure–Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer}, url = {https://m2.mtmt.hu/api/publication/32843044}, author = {Pape, Veronika and Palkó, Roberta and Tóth, Szilárd and Szabó, Miklós J. and Sessler, Judit and Dormán, György and Enyedy, Éva Anna and Soós, Tibor and Szatmári, István and Szakács, Gergely}, doi = {10.1021/acs.jmedchem.2c00076}, journal-iso = {J MED CHEM}, journal = {JOURNAL OF MEDICINAL CHEMISTRY}, volume = {65}, unique-id = {32843044}, issn = {0022-2623}, year = {2022}, eissn = {1520-4804}, pages = {7729-7745}, orcid-numbers = {Pape, Veronika/0000-0001-6589-6950; Dormán, György/0000-0001-7702-2206; Enyedy, Éva Anna/0000-0002-8058-8128; Szatmári, István/0000-0002-8571-5229; Szakács, Gergely/0000-0002-9311-7827} } @article{MTMT:32788926, title = {Efficient Synthesis of Acylated, Dialkyl α-Hydroxy-Benzylphosphonates and Their Anticancer Activity}, url = {https://m2.mtmt.hu/api/publication/32788926}, author = {Varga, Petra Regina and Belovics, Alexandra and Bagi, Péter and Tóth, Szilárd and Szakács, Gergely and Bősze, Szilvia and Szabó, Rita and Drahos, László and Keglevich, György}, doi = {10.3390/molecules27072067}, journal-iso = {MOLECULES}, journal = {MOLECULES}, volume = {27}, unique-id = {32788926}, issn = {1420-3049}, year = {2022}, eissn = {1420-3049}, orcid-numbers = {Bagi, Péter/0000-0002-9043-6435; Tóth, Szilárd/0000-0002-0168-3531; Szakács, Gergely/0000-0002-9311-7827; Bősze, Szilvia/0000-0001-9555-699X; Drahos, László/0000-0001-9589-6652} } @article{MTMT:32540679, title = {Multidrogrezisztens tumorok célzott elpusztítása a P-glikoproteint expresszáló sejtek szelektív vasdepléciójával}, url = {https://m2.mtmt.hu/api/publication/32540679}, author = {Cserepes, Tamás Mihály and Türk, Dóra and Tóth, Szilárd and Pape, Veronika and Gaál, Anikó and Gera, Melinda and Szabó, Judit Eszter and Kucsma, Nóra and Várady, György and Vértessy, Beáta G. and Streli, Christina and Szabó, Pál Tamás and Tóvári, József and Szoboszlai, Norbert and Szakács, Gergely}, journal-iso = {MAGYAR ONKOLÓGIA}, journal = {MAGYAR ONKOLÓGIA}, volume = {65}, unique-id = {32540679}, issn = {0025-0244}, year = {2021}, eissn = {2060-0399}, pages = {15-15}, orcid-numbers = {Cserepes, Tamás Mihály/0000-0003-4816-2618; Szabó, Pál Tamás/0000-0003-2260-4641} } @article{MTMT:31449756, title = {Improved activity and paraptosis-induction of anticancer thiosemicarbazones requires high copper(II) complex stability and slow reduction kinetics}, url = {https://m2.mtmt.hu/api/publication/31449756}, author = {Sonja, Hager and Pape, Veronika and Pósa, Vivien and Bianca, Montsch and Lukas, Uhlik and Szakács, Gergely and Tóth, Szilárd and Nikolett, Jabronka and Bernhard, K. Keppler and Walter, Berger and Christian, R. Kowol and Enyedy, Éva Anna and Petra, Heffeter}, doi = {10.1158/1538-7445.AM2020-1939}, journal-iso = {CANCER RES}, journal = {CANCER RESEARCH}, volume = {80}, unique-id = {31449756}, issn = {0008-5472}, year = {2020}, eissn = {1538-7445}, pages = {1939-1939}, orcid-numbers = {Pape, Veronika/0000-0001-6589-6950; Enyedy, Éva Anna/0000-0002-8058-8128} } @article{MTMT:31305929, title = {High copper complex stability and slow reduction kinetics as key parameters for improved activity, paraptosis induction and impact on drug-resistant cells of anticancer thiosemicarbazones}, url = {https://m2.mtmt.hu/api/publication/31305929}, author = {Sonja, Hager and Pape, Veronika and Pósa, Vivien and Bianca, Montsch and Lukas, Uhlik and Szakács, Gergely and Tóth, Szilárd and Nikolett, Jabronka and Bernhard, K. Keppler and Christian, R. Kowol and Enyedy, Éva Anna and Petra, Heffeter}, doi = {10.1089/ars.2019.7854}, journal-iso = {ANTIOXID REDOX SIGNAL}, journal = {ANTIOXIDANTS & REDOX SIGNALING}, volume = {33}, unique-id = {31305929}, issn = {1523-0864}, year = {2020}, eissn = {1557-7716}, pages = {395-414}, orcid-numbers = {Pape, Veronika/0000-0001-6589-6950; Enyedy, Éva Anna/0000-0002-8058-8128} }