Syntheses and activity of some platinum(IV) complexes with N-methyl derivate of glycine and halogeno ligands against HeLa, K562 cell lines and human PBMC

Four platinum(IV) complexes, trans,trans-dichlorobis(N,N-dimethylglycinato)platinum(IV), trans,trans-[Pt(dmgly)(2)Cl-2] (1) and trans.trans-dibromobis(N,N'-dimethylglycinato)platinum(IV), trans,trans-[Pt(dmgly)(2)Br-2] (2), as well as, trans,trans-dichlorobis(N-methylglycinato)platinum(IV), trans,trans-[Pt(sar)(2)Cl-2] (3) and trans,trans-dibromobis(N-methylglycinato)platinum(IV), trans,trans-[Pt(sar)(2)Br-2] (4) (with configuration index for all complexes OC-6-14), were synthesized and characterized by elemental analysis, infrared and H-1 NMR spectroscopy. In the aim to assess the selectivity in the antitumor action of these complexes, the antiproliferative action of these compounds was determined to human adenocarcinoma HeLa cells; to human myelogenous leukemia K562 cells and to normal immunocompetent cells; i.e., on human PBMC. The details of the crystal structure synthesized trans,trans-[Pt(sar)(2)Br-2] complex were also reported here. In the crystal structure of trans, trans-[Pt(sar)(2)Br-2] the Pt(IV) ion had a deformed octahedral coordination with both N-methylglycinates and bromides bonded trans to one another and with the NPt-Br bond angles of 84.1(4) and 95.9(4)degrees. The trans, trans-[Pt(sar)(2)Br-2] complex molecules form 2D-layers with multiple N-H (...) O and C-H (...) O hydrogen bonds. (c) 2005 Elsevier B.V. All rights reserved