Organometallics · 2020 · 20 citations · 39 references
MedicineMedicinal ChemistryOncologyCancer PharmacologyOrganometallic ChemistryStructure-activity RelationshipsCoordination ChemistryHeterocyclic ChemistryLigand BindingCytotoxicity AssaysLigand Effects On ReactivityMass Spectrometric DetectionPlatinum CompoundsSpectroscopic Characterization Of Metal-ligand Bonds
Eight platinum(II) complexes of the formula [PtCl(arylolefin)(NHC)] (2–9) with varying NHCs and arylolefin chelators have been prepared and analyzed by spectroscopic and spectrometric methods. The study reveals that the binding of the arylolefins is influenced by remote ring substituents and by the NHC spectator ligands. A more strongly donating NHC exhibits an increased trans influence and weakens the olefinic donor notably, which could lead to its premature dissociation. Cytotoxicity studies on four human cancer cell lines indicate that a stronger binding of the arylolefin is more beneficial. The highest cytotoxic effects (IC50 = 0.18–0.70 μM) were observed for the complex [PtCl(Meug)(IMes)] (3), containing a more weakly donating NHC and the strongest arylolefin donor.
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New Colorimetric Cytotoxicity Assay for Anticancer-Drug Screening
Philip Skehan, Ritsa Storeng, Dominic A. Scudiero et al. · JNCI Journal of the National Cancer Institute · 1990 · 9.8K citations
Medicine, Oncology, Pharmacology +10