Exploring the in vitro anticancer activities of Re(I) picolinic acid and its fluorinated complex derivatives on lung...

Fifteen rhenium(I) tricarbonyl complexes of the form fac-[Re(N,O')(CO)₃(X)], where N,O'-bidentate ligand = 2-picolinic acid (Pico); 3,5-difluoropyridine-2-carboxylic acid (Dfpc); 3-trifluoromethyl-pyridine-2-carboxylic acid (Tfpc) and X = H₂O; pyrazole (Pz); pyridine (Py); imidazole (Im); and methanol (CH₃OH) were synthesized using the '2 + 1' mixed ligand approach with an average yield of 84%. The complexes were characterized using the following spectroscopic techniques: IR, ¹H and ¹³C NMR, UV/Vis, and single-crystal X-ray diffraction. The effect of the fluorine atoms on the backbone of the N,O'-bidentate ligand was investigated and a trend was noticed in the carbonyl stretching frequencies: with Pico < Tfpc < Dfpc. The in vitro biological screening on Vero (healthy mammalian), HeLa (cervical carcinoma) and A549 (lung cancer) cells revealed one toxic complex, fac-[Re(Pico)(CO)₃(H₂O)], with respective LC₅₀ values of 9.0 ± 0.9, 15.8 ± 4.9 (SI = 0.570) and 20.9 ± 0.8 (SI = 0.430) μg/mL. As a result, it can be used as a positive control drug of toxicity.