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Publikation

Zmejkovski, B. B.; Pantelić, N.; Filipović, L.; Aranđelović, S.; Radulović, S.; Sabo, T. J.; Kaluđerović, G. N.; In Vitro Anticancer Evaluation of Platinum(II/IV) Complexes with Diisoamyl Ester of (S,S)-ethylenediamine-N,N’-di-2-propanoic Acid Anti-Cancer Agents Med. Chem. 17, 1136-1143, (2017) DOI: 10.2174/1871520616666161207155634

Aims: Platinum(II) and platinum(IV) complexes [PtCln{(S,S)-(i-Am)2eddip}] (n = 2, 4: 1, 2, respectively; (S,S)-(i-Am)2eddip = O,O’-diisoamyl-(S,S)-ethylenediamine-N,N’-di-2-propanoate) were synthesized and characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy and mass spectrometry.Method: Quantum chemical calculations were used to predict formed isomers of 1 and 2. Furthermore, reduction of 2 with ascorbic acid was followed by time-dependant 13C NMR spectroscopy in order to enable assignation of the formed isomers for complex 1. In vitro cytotoxic activity was determined for 1 and 2 on a panel of five human tumor cell lines derived from cervix adenocarcinoma (HeLa), alveolar basal adenocarcinoma (A549), breast adenocarcinoma (MDA-453), colorectal cancer (LS 174), erythromyeloblastoid leukemia (K562), as well as one non-malignant human lung fibroblast cell line (MRC-5), using MTT assay. Result: Both complexes exhibited high (2 against K562: IC50 = 5.4 μM), more active than cisplatin, to moderate activity (1). Both complexes caused considerable decrease of cell number in K562 cells in G1, S and G2 phases, concordantly increasing subpopulation in sub-G1 fraction. Morphological analysis of K562 cell death induced by platinum(II/IV) complexes indicate apoptosis.
Publikation

Zmejkovski, B. B.; Savić, A.; Poljarević, J.; Pantelić, N.; Aranđelović, S.; Radulović, S.; Grgurić-Šipka, S.; Kaluđerović, G. N.; Sabo, T. J.; Synthesis, characterization and in vitro antitumor activity of new palladium(II) complexes with (S,S)-R2edda-type esters Polyhedron 80, 106-111, (2014) DOI: 10.1016/j.poly.2014.02.026

Six palladium(II) complexes with (S,S)-R2edda-type esters ((S,S)-R2edda-type: (S,S)-eddch = (S,S)-ethylenediamine-N,N′-di-2-(3-cyclohexyl)propanoate, R = Me, Et, n-Pr, 1–3; (S,S)-pddch = (S,S)-propylenediamine-N,N′-di-2-(3-cyclohexyl)propanoate, R = Et, n-Pr, 4, 5; and (S,S)-eddip = (S,S)-ethylenediamne-N,N′-di-2-propanoate, R = i-Am, 6) were synthesized, characterized by IR, NMR spectroscopy, ESI-MS and elemental analysis. DFT calculations indicate that in case of 1–4, the most stable isomers are with (S,S)- and (R,S)-configuration of nitrogen atoms, but for complex 6 (R,R)- and (R,S)-N,N′-configured isomers. Furthermore, complex 5 was obtained as (S,S)-N,N′ configured isomer. Cytotoxicity study was performed against human cervical adenocarcinoma (HeLa), human alveolar basal adenocarcinoma (A549) and non-cancerous human fetal lung fibroblast (MRC-5) cell lines using colorimetric MTT assay. From the investigated palladium(II) complexes 2, 3 and 5 exhibited highest cytotoxic potential against HeLa (IC50: 28.5 ± 3.9, 29.5 ± 1.3 and 34.3 ± 3.2, respectively).

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