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 [(n⁶-p-cymene)Ru(pyrithionato)(pta)]PF₆ contains phosphine ligand pta (1,3,5- triaza-7-phosphaadamantane)...
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| Formato: | Articulo |
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2023
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| Acceso en línea: | http://sedici.unlp.edu.ar/handle/10915/154460 |
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I19-R120-10915-154460 |
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I19-R120-10915-1544602023-06-16T20:07:02Z http://sedici.unlp.edu.ar/handle/10915/154460 issn:1420-3049 Exploring pta alternatives in the development of ruthenium–arene anticancer compounds Kljun, Jakob Rebernik, Mihaela Balsa, Lucía Mariana Kladnik, Jerneja Rapuš, Uroš Trobec, Tomaž Sepčić, Kristina Frangež, Robert León, Ignacio Esteban Turel, Iztok 2023 2023-06-16T16:56:05Z en Química Ruthenium Pyrithione Phosphines Anticancer activity Glutathione S-transferase 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 [(n⁶-p-cymene)Ru(pyrithionato)(pta)]PF₆ 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. Centro de Química Inorgánica Articulo Articulo http://creativecommons.org/licenses/by/4.0/ Creative Commons Attribution 4.0 International (CC BY 4.0) application/pdf |
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Universidad Nacional de La Plata |
| institution_str |
I-19 |
| repository_str |
R-120 |
| collection |
SEDICI (UNLP) |
| language |
Inglés |
| topic |
Química Ruthenium Pyrithione Phosphines Anticancer activity Glutathione S-transferase |
| spellingShingle |
Química Ruthenium Pyrithione Phosphines Anticancer activity Glutathione S-transferase Kljun, Jakob Rebernik, Mihaela Balsa, Lucía Mariana Kladnik, Jerneja Rapuš, Uroš Trobec, Tomaž Sepčić, Kristina Frangež, Robert León, Ignacio Esteban Turel, Iztok Exploring pta alternatives in the development of ruthenium–arene anticancer compounds |
| topic_facet |
Química Ruthenium Pyrithione Phosphines Anticancer activity Glutathione S-transferase |
| 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 [(n⁶-p-cymene)Ru(pyrithionato)(pta)]PF₆ 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. |
| format |
Articulo Articulo |
| author |
Kljun, Jakob Rebernik, Mihaela Balsa, Lucía Mariana Kladnik, Jerneja Rapuš, Uroš Trobec, Tomaž Sepčić, Kristina Frangež, Robert León, Ignacio Esteban Turel, Iztok |
| author_facet |
Kljun, Jakob Rebernik, Mihaela Balsa, Lucía Mariana Kladnik, Jerneja Rapuš, Uroš Trobec, Tomaž Sepčić, Kristina Frangež, Robert León, Ignacio Esteban Turel, Iztok |
| author_sort |
Kljun, Jakob |
| title |
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_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_sort |
exploring pta alternatives in the development of ruthenium–arene anticancer compounds |
| publishDate |
2023 |
| url |
http://sedici.unlp.edu.ar/handle/10915/154460 |
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