Synthesis, characterization, toxicity, cytogenetic and in vivo antitumor studies of 1,1-dithiolate Cu(II) complexes with di-, tri-, tetra- amines and 1,3-thiazoles. Structure–activity correlation

A series of new mixed-ligand neutral copper(II) complexes of the general type [Cu(amine)(i-MNT)] and [Cu(tz)(i-MNT)] was prepared and characterized by elemental, spectroscopic methods, μeff, Λμ measurements and molecular modeling studies. The acute toxicity, the cytogenetic and the in vivo antitumor activity of the new complexes, is related to their chemical and physicochemical properties. Among the Cu(II) compounds tested the complex with 2-amino-5-methyl thiazole increases significantly the life span of leukemia P388 bearing mice in vivo.

A series of mixed-ligand neutral Cu(II) complexes with dithiolates, amines or thiazole ligands have been synthesized and the acute toxicity, cytogenetic and in vivo antitumor effects can be related to their chemical and physicochemical properties. The tests showed that the compound 10 can be used as lead compound.Figure optionsDownload as PowerPoint slide