Exploring pta alternatives in the development of ruthenium–arene anticancer compounds

Autores
Kljun, Jakob; Rebernik, Mihaela; Balsa, Lucía Mariana; Kladnik, Jerneja; Rapuš, Uroš; Trobec, Tomaž; Sepčić, Kristina; Frangež, Robert; León, Ignacio Esteban; Turel, Iztok
Año de publicación
2023
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
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
Materia
Química
Ruthenium
Pyrithione
Phosphines
Anticancer activity
Glutathione S-transferase
Nivel de accesibilidad
acceso abierto
Condiciones de uso
http://creativecommons.org/licenses/by/4.0/
Repositorio
SEDICI (UNLP)
Institución
Universidad Nacional de La Plata
OAI Identificador
oai:sedici.unlp.edu.ar:10915/154460
Acceder
id SEDICI_d89ee5ef1ce64245878bb27e18c076b3
oai_identifier_str oai:sedici.unlp.edu.ar:10915/154460
network_acronym_str SEDICI
repository_id_str 1329
network_name_str SEDICI (UNLP)
spelling Exploring pta alternatives in the development of ruthenium–arene anticancer compoundsKljun, JakobRebernik, MihaelaBalsa, Lucía MarianaKladnik, JernejaRapuš, UrošTrobec, TomažSepčić, KristinaFrangež, RobertLeón, Ignacio EstebanTurel, IztokQuímicaRutheniumPyrithionePhosphinesAnticancer activityGlutathione S-transferaseOrganoruthenium 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 Inorgánica2023info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionArticulohttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfhttp://sedici.unlp.edu.ar/handle/10915/154460enginfo:eu-repo/semantics/altIdentifier/issn/1420-3049info:eu-repo/semantics/altIdentifier/doi/10.3390/molecules28062499info:eu-repo/semantics/openAccesshttp://creativecommons.org/licenses/by/4.0/Creative Commons Attribution 4.0 International (CC BY 4.0)reponame:SEDICI (UNLP)instname:Universidad Nacional de La Platainstacron:UNLP2025-09-29T11:40:03Zoai:sedici.unlp.edu.ar:10915/154460Institucionalhttp://sedici.unlp.edu.ar/Universidad públicaNo correspondehttp://sedici.unlp.edu.ar/oai/snrdalira@sedici.unlp.edu.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:13292025-09-29 11:40:03.381SEDICI (UNLP) - Universidad Nacional de La Platafalse
dc.title.none.fl_str_mv Exploring pta alternatives in the development of ruthenium–arene anticancer compounds
title Exploring pta alternatives in the development of ruthenium–arene anticancer compounds
spellingShingle Exploring pta alternatives in the development of ruthenium–arene anticancer compounds
Kljun, Jakob
Química
Ruthenium
Pyrithione
Phosphines
Anticancer activity
Glutathione S-transferase
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
dc.creator.none.fl_str_mv Kljun, Jakob
Rebernik, Mihaela
Balsa, Lucía Mariana
Kladnik, Jerneja
Rapuš, Uroš
Trobec, Tomaž
Sepčić, Kristina
Frangež, Robert
León, Ignacio Esteban
Turel, Iztok
author Kljun, Jakob
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_role author
author2 Rebernik, Mihaela
Balsa, Lucía Mariana
Kladnik, Jerneja
Rapuš, Uroš
Trobec, Tomaž
Sepčić, Kristina
Frangež, Robert
León, Ignacio Esteban
Turel, Iztok
author2_role author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Química
Ruthenium
Pyrithione
Phosphines
Anticancer activity
Glutathione S-transferase
topic Química
Ruthenium
Pyrithione
Phosphines
Anticancer activity
Glutathione S-transferase
dc.description.none.fl_txt_mv 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
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.
publishDate 2023
dc.date.none.fl_str_mv 2023
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
Articulo
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://sedici.unlp.edu.ar/handle/10915/154460
url http://sedici.unlp.edu.ar/handle/10915/154460
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/issn/1420-3049
info:eu-repo/semantics/altIdentifier/doi/10.3390/molecules28062499
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
http://creativecommons.org/licenses/by/4.0/
Creative Commons Attribution 4.0 International (CC BY 4.0)
eu_rights_str_mv openAccess
rights_invalid_str_mv http://creativecommons.org/licenses/by/4.0/
Creative Commons Attribution 4.0 International (CC BY 4.0)
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:SEDICI (UNLP)
instname:Universidad Nacional de La Plata
instacron:UNLP
reponame_str SEDICI (UNLP)
collection SEDICI (UNLP)
instname_str Universidad Nacional de La Plata
instacron_str UNLP
institution UNLP
repository.name.fl_str_mv SEDICI (UNLP) - Universidad Nacional de La Plata
repository.mail.fl_str_mv alira@sedici.unlp.edu.ar
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score 13.070432

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