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| Verfasst von: | Rubbiani, Riccardo [VerfasserIn]  |
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| | Kitanovic, Igor [VerfasserIn] |
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| | Alborzinia, Hamed [VerfasserIn] |
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| | Can, Suzan [VerfasserIn] |
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| | Kitanovic, Ana [VerfasserIn] |
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| | Onambele, Liliane A. [VerfasserIn] |
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| | Stefanopoulou, Maria [VerfasserIn] |
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| | Geldmacher, Yvonne [VerfasserIn] |
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| | Sheldrick, William S. [VerfasserIn] |
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| | Wolber, Gerhard [VerfasserIn] |
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| | Prokop, Aram [VerfasserIn] |
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| | Wölfl, Stefan [VerfasserIn] |
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| | Ott, Ingo [VerfasserIn] |
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| Titel: | Benzimidazol-2-ylidene gold(I) complexes are thioredoxin reductase inhibitors with multiple antitumor properties |
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| Verf.angabe: | Riccardo Rubbiani, Igor Kitanovic, Hamed Alborzinia, Suzan Can, Ana Kitanovic, Liliane A. Onambele, Maria Stefanopoulou, Yvonne Geldmacher, William S. Sheldrick, Gerhard Wolber, Aram Prokop, Stefan Wölfl and Ingo Ott |
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| E-Jahr: | 2010 |
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| Jahr: | November 17, 2010 |
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| Umfang: | 11 S. |
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| Fussnoten: | Gesehen am 22.06.2023 |
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| Titel Quelle: | Enthalten in: Journal of medicinal chemistry |
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| Ort Quelle: | Washington, DC : ACS, 1959 |
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| Jahr Quelle: | 2010 |
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| Band/Heft Quelle: | 53(2010), 24, Seite 8608-8618 |
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| ISSN Quelle: | 1520-4804 |
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| Abstract: | Gold(I) complexes such as auranofin have been used for decades to treat symptoms of rheumatoid arthritis and have also demonstrated a considerable potential as new anticancer drugs. The enzyme thioredoxin reductase (TrxR) is considered as the most relevant molecular target for these species. The here investigated gold(I) complexes with benzimidazole derived N-heterocyclic carbene (NHC) ligands 1a−4a represent a promising class of gold coordination compounds with a good stability against the thiol glutathione. TrxR was selectively inhibited by 1a−4a in comparison to the closely related enzyme glutathione reductase, and all complexes triggered significant antiproliferative effects in cultured tumor cells. More detailed studies on a selected complex (2a) revealed a distinct pharmacodynamic profile including the high increase of reactive oxygen species formation, apoptosis induction, strong effects on cellular metabolism (related to cell surface properties, respiration, and glycolysis), inhibition of mitochondrial respiration and activity against resistant cell lines. |
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| DOI: | doi:10.1021/jm100801e |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.1021/jm100801e |
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| | DOI: https://doi.org/10.1021/jm100801e |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| K10plus-PPN: | 1850803161 |
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| Verknüpfungen: | → Zeitschrift |
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Benzimidazol-2-ylidene gold(I) complexes are thioredoxin reductase inhibitors with multiple antitumor properties / Rubbiani, Riccardo [VerfasserIn]; November 17, 2010 (Online-Ressource)
