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

KLJUN, JAKOB; REBERNIK, MIHAELA; BALSA, L.M.; JERNEJA KLADNIK; UROS RAPUS; TOMAZ TROBEC; KRISTINA SEPCIC; ROBERT FRANGEZ; LEON I.E; TUREL I

MOLECULES

MOLECULAR DIVERSITY PRESERVATION INTERNATIONAL-MDPI

Lugar: Basel; Año: 2023

1420-3049

Organoruthenium pyrithione (1-hydroxypyridine-2-thione) complexes have been shownin our recent studies to be a promising family of compounds for development of new anticancerdrugs. The complex [(6-p-cymene)Ru(pyrithionato)(pta)]PFcontains phosphine ligand pta (1,3,5triaza-7-phosphaadamantane)as a functionality that improves the stability of the complex and itsaqueous solubility. Here, we report our efforts to find pta alternatives and discover new structuralelements to improve the biological properties of ruthenium anticancer drugs. The pta ligand wasreplaced 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.