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Potent and selective anticancer activity of half-sandwich ruthenium and osmium complexes with modified curcuminoid ligands

Noemi Pagliaricci, Riccardo Pettinari, F. Marchetti, Claudio Pettinari, Loredana Cappellacci, Alessia Tombesi, Massimiliano Cuccioloni, Mouna Hadiji, Paul J. Dyson

2022Dalton Transactions21 citationsDOIOpen Access PDF

Abstract

] 5-8 are salts obtained when the chloride ligand is replaced by the PTA ligand. Stability studies performed on 1-8 in DMSO-PBS under physiological conditions (pH = 7.4) indicate that the complexes remain intact. The complexes exhibit potent and selective cytotoxic activity against an ovarian carcinoma cell line and its cisplatin-resistant form (A2780 and A2780cis), and non-cancerous human embryonic kidney (HEK293T) cells. To define the structure-activity relationships (SAR), the compounds have been compared with other Ru(II) and Os(II) complexes with curcuminoid ligands previously reported. SAR data reveal that the bisdemethoxycurcumin complexes are generally more active and selective than analogous curcumin-containing complexes.

Topics & Concepts

ChemistryCurcuminoidRutheniumLigand (biochemistry)StereochemistryOsmiumCurcuminMedicinal chemistryOrganic chemistryBiochemistryReceptorCatalysisMetal complexes synthesis and propertiesMetal-Organic Frameworks: Synthesis and ApplicationsCurcumin's Biomedical Applications
Potent and selective anticancer activity of half-sandwich ruthenium and osmium complexes with modified curcuminoid ligands | Litcius