Secondary ligand effects on the cytotoxicity of several Casiopeína's group II compounds

Abstract

The aim of this study is to identify the influence of the ligand aminoacidato on the antiproliferative activity against human tumor cell lines HeLa, HCT-15 and SKL-U through the analysis of a set of Cu(II) coordination compounds with general formula [Cu(4,7- dimethyl-1,10-phenanthroline)(N-O)]NO 3where N-O represents several essential aminoacids. Results show that the hydrophobicity of the amino acid ligands increases the cellular uptake of copper (II) in HeLa tumor cell line, however, the increase of copper concentration inside the cell is not enough to produce significant changes in antiproliferative activity in this tumor cell line. Thus, the substituents on diimine ligand apparently play the stronger role to control the activity of these complexes. Also molecular structures of compounds 2 (Cas IIala) and 4 (Cas IInva) are presented. © 2012, Sociedad Química de México.