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Exploring pta Alternatives in the Development of Ruthenium-Arene Anticancer Compounds.
Kljun, Jakob; Rebernik, Mihaela; Balsa, Lucía M; Kladnik, Jerneja; Rapus, Uros; Trobec, Tomaz; Sepcic, Kristina; Frangez, Robert; León, Ignacio E; Turel, Iztok.
Affiliation
  • Kljun J; Faculty of Chemistry and Chemical Technology, University of Ljubljana, Vecna pot 113, SI-1000 Ljubljana, Slovenia.
  • Rebernik M; Faculty of Chemistry and Chemical Technology, University of Ljubljana, Vecna pot 113, SI-1000 Ljubljana, Slovenia.
  • Balsa LM; CEQUINOR (UNLP, CCT-CONICET La Plata, Asociado a CIC), Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Blvd. 120 N°1465, La Plata 1900, Argentina.
  • Kladnik J; Faculty of Chemistry and Chemical Technology, University of Ljubljana, Vecna pot 113, SI-1000 Ljubljana, Slovenia.
  • Rapus U; Faculty of Chemistry and Chemical Technology, University of Ljubljana, Vecna pot 113, SI-1000 Ljubljana, Slovenia.
  • Trobec T; Institute of Preclinical Sciences, Veterinary Faculty, University of Ljubljana, Gerbiceva 60, SI-1000 Ljubljana, Slovenia.
  • Sepcic K; Department of Biology, Biotechnical Faculty, University of LjubljanaJamnikarjeva 101, SI-1000 Ljubljana, Slovenia.
  • Frangez R; Institute of Preclinical Sciences, Veterinary Faculty, University of Ljubljana, Gerbiceva 60, SI-1000 Ljubljana, Slovenia.
  • León IE; CEQUINOR (UNLP, CCT-CONICET La Plata, Asociado a CIC), Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Blvd. 120 N°1465, La Plata 1900, Argentina.
  • Turel I; Faculty of Chemistry and Chemical Technology, University of Ljubljana, Vecna pot 113, SI-1000 Ljubljana, Slovenia.
Molecules ; 28(6)2023 Mar 09.
Article in En | MEDLINE | ID: mdl-36985471
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 [(η6-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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Organometallic Compounds / Phosphines / Ruthenium / Coordination Complexes / Antineoplastic Agents Language: En Journal: Molecules Journal subject: BIOLOGIA Year: 2023 Document type: Article Affiliation country: Slovenia Country of publication: Switzerland
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Organometallic Compounds / Phosphines / Ruthenium / Coordination Complexes / Antineoplastic Agents Language: En Journal: Molecules Journal subject: BIOLOGIA Year: 2023 Document type: Article Affiliation country: Slovenia Country of publication: Switzerland