Abstract: In this contribution we report the synthesis, characterization and in vitro anticancer activity of novel cyclometalated 4-phenylthiazole-derived ruthenium(II) (2a–e) and osmium(II) (3a–e) complexes. Formation and sufficient purity of the complexes were unambigiously confirmed by 1H-, 13C- and 2D-NMR techniques, X-ray diffractometry, HRMS and elemental analysis. The binding preferences of these cyclometalates to selected amino acids and to DNA models including G-quadruplex structures were analyzed. Additionally, their stability and behaviour in aqueous solutions was determined by UV-Vis spectroscopy. Their cellular accumulation, their ability of inducing apoptosis, as well as their interference in the cell cycle were studied in SW480 colon cancer cells. The anticancer potencies were investigated in three human cancer cell lines and revealed IC50 values in the low micromolar range, in contrast to the biologically inactive ligands.
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With palladium(II) trifluoroacetate; silver carbonate; glyoxal bis(N-methyl-N-phenylhydrazone); In dimethyl sulfoxide; at 80℃; for 2h;
General procedure: To a mixture of arylcarboxylic acid (0.20 mmol), Ag2CO3 (165 mg, 0.60 mmol), Pd(TFA)2 (5.0 mg, 0.015 mmol, 7.5 mol %), and ligand 1d (4.0 mg, 0.015 mmol, 7.5 mol %) in DMSO (1.0 mL) was addedarylboroxin (0.40 mmol) at room temperature under an atmosphere of air.After the mixture was stirred at 80?C for 2 h, the mixture was diluted withethyl acetate and water. The organic layer was washed with brine, dried overMgSO4, and concentrated under reduced pressure. The residue was purified by silica gel chromatography (hexane/EtOAc = 20:1).
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