Exploring pta Alternatives in the Development of Ruthenium–Arene Anticancer Compounds

Organoruthenium pyrithione (1-hydroxypyridine-2-thione) complexes have been shown in our recent studies to be a promising family of compounds for development of new anticancer drugs. The complex [(η(6)-p-cymene)Ru(pyrithionato)(pta)]PF(6) contains phosphine ligand pta (1,3,5-triaza-7-phosphaadamanta...

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Autores principales: Kljun, Jakob, Rebernik, Mihaela, Balsa, Lucía M., Kladnik, Jerneja, Rapuš, Uroš, Trobec, Tomaž, Sepčić, Kristina, Frangež, Robert, León, Ignacio E., Turel, Iztok
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
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Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10058425/
https://www.ncbi.nlm.nih.gov/pubmed/36985471
http://dx.doi.org/10.3390/molecules28062499
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author Kljun, Jakob
Rebernik, Mihaela
Balsa, Lucía M.
Kladnik, Jerneja
Rapuš, Uroš
Trobec, Tomaž
Sepčić, Kristina
Frangež, Robert
León, Ignacio E.
Turel, Iztok
author_facet Kljun, Jakob
Rebernik, Mihaela
Balsa, Lucía M.
Kladnik, Jerneja
Rapuš, Uroš
Trobec, Tomaž
Sepčić, Kristina
Frangež, Robert
León, Ignacio E.
Turel, Iztok
author_sort Kljun, Jakob
collection PubMed
description Organoruthenium pyrithione (1-hydroxypyridine-2-thione) complexes have been shown in our recent studies to be a promising family of compounds for development of new anticancer drugs. The complex [(η(6)-p-cymene)Ru(pyrithionato)(pta)]PF(6) contains phosphine ligand pta (1,3,5-triaza-7-phosphaadamantane) as a functionality that improves the stability of the complex and its aqueous solubility. Here, we report our efforts to find pta alternatives and discover new structural elements to improve the biological properties of ruthenium anticancer drugs. The pta ligand was replaced by a selection of phosphine, phosphite, and arsine ligands to identify new functionalities, leading to improvement in inhibitory potency towards enzyme glutathione S-transferase. In addition, cytotoxicity in breast, bone, and colon cancers was investigated.
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spelling pubmed-100584252023-03-30 Exploring pta Alternatives in the Development of Ruthenium–Arene Anticancer Compounds Kljun, Jakob Rebernik, Mihaela Balsa, Lucía M. Kladnik, Jerneja Rapuš, Uroš Trobec, Tomaž Sepčić, Kristina Frangež, Robert León, Ignacio E. Turel, Iztok Molecules Article Organoruthenium pyrithione (1-hydroxypyridine-2-thione) complexes have been shown in our recent studies to be a promising family of compounds for development of new anticancer drugs. The complex [(η(6)-p-cymene)Ru(pyrithionato)(pta)]PF(6) contains phosphine ligand pta (1,3,5-triaza-7-phosphaadamantane) as a functionality that improves the stability of the complex and its aqueous solubility. Here, we report our efforts to find pta alternatives and discover new structural elements to improve the biological properties of ruthenium anticancer drugs. The pta ligand was replaced by a selection of phosphine, phosphite, and arsine ligands to identify new functionalities, leading to improvement in inhibitory potency towards enzyme glutathione S-transferase. In addition, cytotoxicity in breast, bone, and colon cancers was investigated. MDPI 2023-03-09 /pmc/articles/PMC10058425/ /pubmed/36985471 http://dx.doi.org/10.3390/molecules28062499 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Kljun, Jakob
Rebernik, Mihaela
Balsa, Lucía M.
Kladnik, Jerneja
Rapuš, Uroš
Trobec, Tomaž
Sepčić, Kristina
Frangež, Robert
León, Ignacio E.
Turel, Iztok
Exploring pta Alternatives in the Development of Ruthenium–Arene Anticancer Compounds
title Exploring pta Alternatives in the Development of Ruthenium–Arene Anticancer Compounds
title_full Exploring pta Alternatives in the Development of Ruthenium–Arene Anticancer Compounds
title_fullStr Exploring pta Alternatives in the Development of Ruthenium–Arene Anticancer Compounds
title_full_unstemmed Exploring pta Alternatives in the Development of Ruthenium–Arene Anticancer Compounds
title_short Exploring pta Alternatives in the Development of Ruthenium–Arene Anticancer Compounds
title_sort exploring pta alternatives in the development of ruthenium–arene anticancer compounds
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10058425/
https://www.ncbi.nlm.nih.gov/pubmed/36985471
http://dx.doi.org/10.3390/molecules28062499
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