European Journal of Medicinal Chemistry · 2011 · 81 citations · 20 references
PharmacyChemistryMedicinal ChemistryCancer PharmacologyChemotherapyStructure-activity RelationshipsAntineoplastic Drug ClassesCoordination ChemistryCytotoxic ChemotherapyLigand BindingChemical Structure-activity RelationshipsCytotoxicity AssaysMetalloid ComplexesNon-small Cell Lung Cancer TreatmentOctanol-water Partition CoefficientOrganometallic Anticancer AgentsPlatinum CompoundsX-ray Diffraction Analysis
A series of six novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes was synthesized and characterized in detail by elemental analysis, FT-IR, ESI-MS, HPLC, multinuclear ((1)H, (13)C, (15)N, (195)Pt) NMR spectroscopy and in one case by X-ray diffraction. Cytotoxic properties of the complexes were evaluated in four human tumor cell lines originating from ovarian carcinoma (CH1 and SK-OV-3), colon carcinoma (SW480) and non-small cell lung cancer (A549) by means of the MTT colorimetrical assay. In addition, their octanol/water partition coefficients (log P values) were determined. Remarkably the most active (and also most lipophilic) compounds, having 4-propyloxy-4-oxobutanoato and 4-(2-propyloxy)-4-oxobutanoato axial ligands, showed IC(50) values down to the low nanomolar range.
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