Stereospecific ligands and their complexes. Part X: Synthesis, characterization and in vitro antitumoral activity of platinum(IV) complexes with O,O′-dialkyl-(S,S)-ethylenediamine-N,N′-di-2-(4-methyl) pentanoate ligands

摘要

Synthesis of four new platinum(IV) complexes 1-4, with bidentate N,N′-ligand precursors O,O′-dialkyl esters (alkyl = ethyl, n-propyl, n-butyl and n-pentyl), of (S,S)-ethylenediamine-N,N′-di-2-(4-methyl) pentanoic acid dihydrochloride [(S,S)-H _4eddl]Cl _2 were reported. The composition of the novel platinum complexes was determined by elemental analysis and characterizations were performed by infrared, ~1H and ~(13)C NMR spectroscopy. DFT calculations indicate formation one (R,R) from three possible diastereoisomers (S,S; R,S). Complexes 1-4 displayed potent anticancer activity. IC 50 values range from 0.74 to 70 μM, against tested cell lines, except for CLL cells. The antitumoral activity of 2-4 was found to be considerably stronger to Jurkat and K562. Cell cycle analysis of cell lines showed G1 arrest in the presence of analyzed complexes.