Dalton Transactions · 2017 · 34 citations · 59 references
MedicineMedicinal ChemistryPharmacologyApoptosisChemotherapyDrug DiscoveryApoptosis PharmacologyApoptosis ResistanceCytotoxic ChemotherapyLigand BindingLigand-based DesignAnti-apoptotic AgentsAnticancer ActivityAnticancer ChemotherapyCancer Targeting LigandsCell Death AssaysCytotoxicity AssaysMetallodrug DesignPlatinum Compounds
value range as low as 10-0.8 μM. Several biological assays were carried out to gain insight into the mechanism of action. Cell death by apoptosis and pH-independent action has been demonstrated. In addition, a selective cytotoxicity profile for tumoral cells over non-tumoral cells has been identified. Importantly, for the key candidates no loss of activity was observed when applied to the Pt-resistant A2780R, which highlights the potential utility of the bis-phospinoamine scaffold as an easily-tunable auxiliary ligand core in both drug discovery and subsequently a logical design of new anticancer metal-containing drugs. The complexes are characterised by NMR spectroscopy, mass spectrometry and single-crystal X-ray diffraction.
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NKP-1339, the first ruthenium-based anticancer drug on the edge to clinical application
Robert Trondl, Petra Heffeter, Christian R. Kowol et al. · Chemical Science · 2014 · 659 citations · Full text
Medicine, Oncology, Pharmacology +14