Correlations between the in vitro antiproliferative activity, structure and thermal stability of some macrocyclic dinuclear Cu(II) complexes
2014
Seven macrocyclic dinuclear Cu(II) complexes with tpmc =
N,N',N",N'"-tetrakis(2-pyridylmethyl)-1,4,8,11-tetraazacyclotetradecane of
coordination formulae [Cu2tpmc](ClO4)4 (1), [Cu2(X)tpmc](ClO4)3•nH2O, X= F-,
n = 0 (2), X = Cl-, n = 1 (3), X = Br-, n = 0 (4), X= I-, n = 1 (5), X =
NO2-, n = 0 (6), [Cu2(NCS)2tpmc](ClO4)2 (7) were evaluated for their
cytotoxic activity against human cervix adenocarcinoma (HeLa), human melanoma
(Fem-x) and human colon carcinoma (LS174) cell lines. The results were
compared with the corresponding data for the
cis-dichlorido-diammineplatinum(II) (CDDP) as referent cytostatic together
with the free ligands and solvent dimethyl sulfoxide (DMSO) as controls. The
complexes showed considerable antiproliferative effect, although
significantly less than CDDP. The thermal decomposition pattern of the
complexes was determined by simultaneous TG/DSC measurements. The thermal
stability of the compounds 2-7 followed the trend of their antiproliferative
activity against HeLa cell line, as well as their corresponding stability
constants. The highest thermal stability and cytotoxicity belonged to complex
[Cu2tpmc](ClO4)4, with no anionic co-ligand. Complex [Cu2(NO2)tpmc](ClO4)3
exhibited a selective cytotoxicity against LS174 cells, at the level of the
most active [Cu2tpmc](ClO4)4. [Projekat Ministartsva nauke Republike Srbije,
br. 172014 i br. 175011]
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