SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF 5-PYRAZOLONE DERIVATIVES AND THERE CU(II), NI(II), CO(II) AND V(V) COMPLEXES

• Main Authors: Eena Mihaela PAHONTU, Donald POIRIER, Aurelian GULEA
• Format: Article
• Language: English
• Published: Academy of Sciences of Moldova 2018-07-01
• Series: Akademos: Revista de Ştiinţă, Inovare, Cultură şi Artă
• Subjects: 5-pyrazolones; thiosemicarbazones; metal complexes; antiproliferative agents; hl-60 leukemia cells
• Online Access: http://akademos.asm.md/files/38-47.pdf

Complex combinations of Cu(II), Ni(II), Co(II) and V(V) with thiosemicarbazone derivatives of 1-phenyl-3-methyl-4-benzoyl-5-pyrazolone-4-R-thiosemicarbazone (where R = CH3, C2H5, C6H5, C5H5N) were synthesized. The characterization of the newly formed compounds was done by 1H NMR, 13C NMR, IR, UV–Vis spectroscopy, elemental analysis, molar electric conductibility, magnetic susceptibility measurements and thermal analysis. For the copper(II) complexes metal–ligand bonding parameters have been evaluated from the EPR spectra. In addition, the structures of the ligands ( HL1-3) and its copper(II) (1, 6, 8, 12), nickel(II) (3, 13) and vanadium(V) (9) complexes were determined by single-crystal X-ray diffraction. The composition of the coordination polyhedron of the central atom in complexes is different. The complexes and ligands were tested for their in vitro antiproliferative activity on human leukemia HL-60. Antiproliferative activity of copper(II) complexes (1, 2, 5 - 8, 11, 12, 15, 16 ) at 10 µM is similar to doxorubicin, used in medical practice as antileukemia drug. The IC50 values were found to be 0.24 μM for complex 2, 0.3 μM for complex 6 and 0.36 μM for complex 11 reveal the potential antiproliferative of these compounds.