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SYNTHESIS AND CHARACTERIZATION OF SOME METAL COMPLEXES WITH A LIGAND DERIVED FROM NOVEL 1,2,3-TRIAZOLE DERIVATIVE AND EVALUATION OF THEIR ANTICANCER ACTIVITIES AND THE PERCENT OF uPA INHIBITION IN VITRO
Pages : [1] - [27]
Received : December 24, 2014; Revised June 12, 2015
Communicated by : Professor Ana Rosa Silva
Abstract
A new ligand, 2-(5-methyl-1-p-tolyl-1H-1,2,3-triazole-4-carbonyl)-N-phenylhydrazine-arbothioamide and its structure has been confirmed by elemental analysis, IR, mass, and NMR spectra. Mass spectra is also used to confirm the proposed formula and the possible fragments resulted from fragmentation of ligand. Its Co(II), Ni(II), Cu(II), Zn(II), Mn(II), Fe(III), and Ag(I) complexes have been prepared, characterized and their structures have been verified on the basis of analytical data, molar conductance, IR, NMR, UV-vis and magnetic measurements. The molar conductance data reveal that all complexes are non-electrolytes, except complexes 4 and 5 are ionic in nature. IR spectra show that ligand is coordinated to the metal ions in a tridentate manner with ONS atoms or tetradentate through ONS atoms beside the 1,2,3-triazole ring–N. The geometrical structures of these complexes are octahedral. The biological activities of ligand and its complexes have been tested in vitro, where cytotoxicity activity and the percent of Urokinase plasminogen activator (uPA) inhibition of them against three different human tumor cell lines including breast cancer cell line MCF-7, liver cancer cell line HepG2, and lung carcinoma A549 that may act through uPA inhibition were evaluated. The results showed that the metal complexes are more anticancer activity than the free ligand. This may be due to coordination and chelating trends to make metal complexes act as more powerful and potent anticancer agents, thus inhibiting the growth of the uPA. The Zn(II) complex (8) has the best complex exerting a significant cytotoxic compared to doxorubicin (the commonly used anticancer drug).
Keywords
1,2,3-triazole, metal complexes, antiproliferative and human cancer cell lines.