Abstract
Preparations of copper(II) and palladium(II) complexes of 4-amino-5-methylthio-3-(2-pyridyl)-1,2,4-triazole (L 1) and the copper(II) complex of 1,4-dihydro-4-amino-3-(2-pyridyl)-5-thioxo-1,2,4-triazole (HL) are described. These complexes have been characterized by means of spectroscopy and microanalysis. Molecular structures of HL ( 1), [CuCl 2(H 2L)]Cl·2H 2O ( 2a), cis-[CuCl 2(L 1)] ( 3), and cis-[PdCl 2(L 1)] ( 4) have been determined by single-crystal X-ray diffraction. The HL ligand acts as a N, S bidentate through the thioxo moiety and the exo-amino group whilst the ligand L 1 forms N, N coordination complexes through the pyridine and triazole nitrogen atoms. Speciation in solution of the systems Cu/HL and Cu/L 1 have been determined by means of potentiometry and spectrophotometry as well as for the Cu/L 1/A (HA=glycine) system in order to determine species present at physiological pH. Antiproliferative activity of these complexes and their ligands was evaluated, using the AlamarBlue™ Assay, on normal human fibroblasts (HF) and human fibrosarcoma tumor (HT1080) cells. The copper compounds cis-[CuCl 2(H 2L)]Cl and cis-[CuCl 2(L 1)] exerted significant antiproliferative activity of both normal and neoplastic cells; although dose–response experiments revealed that the HT1080 cell line was more sensitive to the tested drugs than normal fibroblasts.
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