6533b7d5fe1ef96bd12646d4

RESEARCH PRODUCT

Synthesis, spectroscopic characterization and antiproliferative activity of two platinum(II) complexes containing N-donor heterocycles

Giuseppe BrunoMaria Assunta GirasoloFrancesco NicolòSimona RubinoGiancarlo StoccoSantino OrecchioLuisa TesoriereV. Di StefanoAlessandro Attanzio

subject

CisplatinLigandChemistryStereochemistrychemistry.chemical_elementPhosphatidylserineIn vitroMononuclear platinum complexes Heterocyclic nitrogen Dimethylsulfoxide Antitumor activityAntitumor activity Dimethylsulfoxide Heterocyclic nitrogen Mononuclear platinum complexesDimethylsulfoxide Heterocyclic nitrogen Mononuclear platinum complexesInorganic Chemistrychemistry.chemical_compoundMembraneSettore CHIM/03 - Chimica Generale E InorganicaMaterials ChemistryProton NMRmedicineMoleculePhysical and Theoretical ChemistryPlatinumAntitumor activitymedicine.drug

description

Abstract Novel mononuclear complexes of Pt(II), cis -[PtCl 2 (DMSO)HL]·2DMSO ( 1 ), where HL = 7-amino-2-(methylthio)[1,2,4]triazolo[1,5- a ]pyrimidine-6-carboxylic acid and Pt(bdt)Cl 2 ( 2 ), where bdt = [2,4-bis(5,6-diphenyl-1,2,4-triazin-3yl)-pyridine] have been synthesized and characterized by elemental analysis, IR and 1 H NMR spectroscopy and X-ray crystallography diffraction analyses. The molecular structure of ( 1 ) shows that Pt(II) ion has a square planar geometry with N(3) bonded heterocycle ligand, two cis chloride anions and S-bonded dimethylsulfoxide. The antiproliferative activity of complexes ( 1 ) and ( 2 ) has been tested in vitro against HepG2 human hepatoma cells and non-malignant human-derived hepatic cells (Chang). Complex ( 1 ), cis -[PtCl 2 (DMSO)HL]·2DMSO, was effective inducer of apoptotic death on HepG2 cells and its cytotoxic activity was higher than that exerted by cisplatin. Apoptosis effect was associated with externalization of plasma membrane phosphatidylserine.

yearjournalcountryeditionlanguage
2014-07-01Inorganica Chimica Acta
https://doi.org/10.1016/j.ica.2014.03.028