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Autor Nach Häufigkeit alphabetisch sortiert
- Kaluđerović, G. N. (2)
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- Zmejkovski, B. B. (1)

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Publikation

Pantelić, N. ?.; Lerbs, M.; Wolf, K.; Wessjohann, L. A.; Kaluđerović, G. N.; In vitro anticancer evaluation of novel triphenyltin(IV) compounds with some N-acetyl-S-(naphthoquinone)cysteine derivatives J. Serb. Chem. Soc. 84, 1119-1127, (2019) DOI: 10.2298/JSC190322032P

Triphenyltin(IV) compounds with naphthoquinone derivatives containing N-acetylcysteine, N-acetyl-S-(1,2-dion-4-naphthyl)cysteine (1,2-NQC), 1, and N-acetyl-S-(1,4-dion-2-naphthyl)cysteine (1,4-NQC), 2, were synthesized and characterized by elemental microanalysis, IR, multinuclear (1H, 13C, 119Sn) NMR spectroscopy as well as HR-ESI mass spectrometry. With the aim of in vitro anticancer activity determination of ligand precursors and novel synthesized organotin(IV) compounds against human cervix adenocarcinoma (HeLa), human colon carcinoma (HT-29), and melanoma carcinoma cell line (B16F10), MTT colorimetric assay method was applied. The results indicate that synthesized compounds exhibited remarkable antiproliferative activity toward all tested cell lines with IC50 in the range of 0.17 to 0.87 μM. Complex 1 showed the greatest activity against HT-29 cells, with IC50 value of 0.21 ± 0.01 μM, 119 times better than cisplatin, while complex 2 demonstrated the highest activity toward HeLa cells, IC50 = 0.17 ± 0.01 μM, which is ~26 times better than cisplatin.

Publikation

Pantelić, N.; Zmejkovski, B. B.; Stanojković, T. P.; Jeftić, V. V.; Radić, G. P.; Trifunović, S. R.; Kaluđerović, G. N.; Sabo, T. J.; Synthesis and high in vitro cytotoxicity of some (S,S)-ethylenediamine-N,N’-di-2-propanoate dihydrochloride esters J. Serb. Chem. Soc. 79, 649-658, (2014) DOI: 10.2298/JSC130512022P

A novel (S,S)-R2eddip ester, O,O′-diisopentyl-(S,S)-ethylenediamine-N,N′-di-2-propanoate dihydrochloride (1) was synthesized and characterized by IR, 1H- and 13C-NMR spectroscopy, mass spectroscopy and elemental analysis. In vitro antitumor action of 1, and two more R2eddip esters, dialkyl (S,S)-ethylenediamine-N,N′-di-2-propanoate dihydrochlorides, obtained before (alkyl = n-Bu or n-Pe, 2 and 3, respectively), was determined against cervix adenocarcinoma (HeLa), human melanoma (Fem-x), human chronic myelogenous leukemia (K562) cells, and a non-cancerous cell line human embryonic lung fibroblast (MRC-5), using the microculture tetrazolium test MTT assay. Esters 1–3 showed higher cytotoxicity and better selectivity in comparison to cisplatin, used as reference compound. The highest activity was expressed by 1, with IC50(Fem-x) value of 1.51±0.09 μM.