TY  - JOUR
AU  - Filipović, Nenad R.
AU  - Bjelogrlić, Snežana K.
AU  - Pelliccia, Sveva
AU  - Jovanović, Vesna B.
AU  - Kojić, Milan
AU  - Sencanski, Milan
AU  - La Regina, Giuseppe
AU  - Silvestri, Romano
AU  - Muller, Christian D.
AU  - Todorović, Tamara R.
PY  - 2020
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1407
AB  - Triapine, the most studied alpha-N-heterocyclic thiosemicarbazone, revealed potent activity against advanced leukemia, but was ineffective against a variety of solid tumors. Moreover, methemoglobinemia, which is a side effect of triapine administration, may limits all clinical application. To enhance anticancer activity and reduce side effects, we applied an isosteric replacement of sulfur to selenium atom was performed by synthesis and characterization of selenium triapine analog, 3-aminopyridine-2-carboxaldehyde selenosemicarbazone (selenotriapine). Compared to triapine, selenotriapine revealed superior pro-apoptotic activity with activation of intrinsic apoptotic pathway in both human monocytic leukemia (THP-1) and mammary adenocarcinoma (MCF-7) cell lines. For MCF-7 2-D cultures, selenotriapine induced notable increase in mitochondrial superoxide radical generation and dissipation of mitochondrial transmembrane potential. A significant delay in growth of MCF-7 spheroids (3-D culture) was accompanied by phenotypic stem cell reprogramming (Oct-4 expression). Additionally, selenotriapine demonstrated a very low toxicity profile as compared to triapine, confirmed over alleviated extent of methemoglobin formation and higher IC50 value in brine shrimp cytotoxicity assay.
PB  - Elsevier, Amsterdam
T2  - Arabian Journal of Chemistry
T1  - Selenotriapine - An isostere of the most studied thiosemicarbazone with pronounced pro-apoptotic activity, low toxicity and ability to challenge phenotype reprogramming of 3-D mammary adenocarcinoma tumors
EP  - 1489
IS  - 1
SP  - 1466
VL  - 13
DO  - 10.1016/j.arabjc.2017.11.017
ER  - 

@article{
author = "Filipović, Nenad R. and Bjelogrlić, Snežana K. and Pelliccia, Sveva and Jovanović, Vesna B. and Kojić, Milan and Sencanski, Milan and La Regina, Giuseppe and Silvestri, Romano and Muller, Christian D. and Todorović, Tamara R.",
year = "2020",
abstract = "Triapine, the most studied alpha-N-heterocyclic thiosemicarbazone, revealed potent activity against advanced leukemia, but was ineffective against a variety of solid tumors. Moreover, methemoglobinemia, which is a side effect of triapine administration, may limits all clinical application. To enhance anticancer activity and reduce side effects, we applied an isosteric replacement of sulfur to selenium atom was performed by synthesis and characterization of selenium triapine analog, 3-aminopyridine-2-carboxaldehyde selenosemicarbazone (selenotriapine). Compared to triapine, selenotriapine revealed superior pro-apoptotic activity with activation of intrinsic apoptotic pathway in both human monocytic leukemia (THP-1) and mammary adenocarcinoma (MCF-7) cell lines. For MCF-7 2-D cultures, selenotriapine induced notable increase in mitochondrial superoxide radical generation and dissipation of mitochondrial transmembrane potential. A significant delay in growth of MCF-7 spheroids (3-D culture) was accompanied by phenotypic stem cell reprogramming (Oct-4 expression). Additionally, selenotriapine demonstrated a very low toxicity profile as compared to triapine, confirmed over alleviated extent of methemoglobin formation and higher IC50 value in brine shrimp cytotoxicity assay.",
publisher = "Elsevier, Amsterdam",
journal = "Arabian Journal of Chemistry",
title = "Selenotriapine - An isostere of the most studied thiosemicarbazone with pronounced pro-apoptotic activity, low toxicity and ability to challenge phenotype reprogramming of 3-D mammary adenocarcinoma tumors",
pages = "1489-1466",
number = "1",
volume = "13",
doi = "10.1016/j.arabjc.2017.11.017"
}

Filipović, N. R., Bjelogrlić, S. K., Pelliccia, S., Jovanović, V. B., Kojić, M., Sencanski, M., La Regina, G., Silvestri, R., Muller, C. D.,& Todorović, T. R.. (2020). Selenotriapine - An isostere of the most studied thiosemicarbazone with pronounced pro-apoptotic activity, low toxicity and ability to challenge phenotype reprogramming of 3-D mammary adenocarcinoma tumors. in Arabian Journal of Chemistry
Elsevier, Amsterdam., 13(1), 1466-1489.
https://doi.org/10.1016/j.arabjc.2017.11.017

Filipović NR, Bjelogrlić SK, Pelliccia S, Jovanović VB, Kojić M, Sencanski M, La Regina G, Silvestri R, Muller CD, Todorović TR. Selenotriapine - An isostere of the most studied thiosemicarbazone with pronounced pro-apoptotic activity, low toxicity and ability to challenge phenotype reprogramming of 3-D mammary adenocarcinoma tumors. in Arabian Journal of Chemistry. 2020;13(1):1466-1489.
doi:10.1016/j.arabjc.2017.11.017 .

Filipović, Nenad R., Bjelogrlić, Snežana K., Pelliccia, Sveva, Jovanović, Vesna B., Kojić, Milan, Sencanski, Milan, La Regina, Giuseppe, Silvestri, Romano, Muller, Christian D., Todorović, Tamara R., "Selenotriapine - An isostere of the most studied thiosemicarbazone with pronounced pro-apoptotic activity, low toxicity and ability to challenge phenotype reprogramming of 3-D mammary adenocarcinoma tumors" in Arabian Journal of Chemistry, 13, no. 1 (2020):1466-1489,
https://doi.org/10.1016/j.arabjc.2017.11.017 . .

TY  - JOUR
AU  - Bjelogrlić, Snežana K.
AU  - Todorović, Tamara R.
AU  - Kojić, Milan
AU  - Sencanski, Milan
AU  - Nikolić, Milan
AU  - Visnjevac, Aleksandar
AU  - Araskov, Jovana
AU  - Miljković, Marija
AU  - Muller, Christian D.
AU  - Filipović, Nenad R.
PY  - 2019
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1197
AB  - Anticancer activity of Pd complexes 1-5 with bidentate N-heteroaromatic hydrazone ligands was investigated on human acute monocytic leukemia (THP-1; cells in a suspension) and human mammary adenocarcinoma (MCF-7; two-dimensional layer and three-dimensional spheroid tumor model) cell lines. For the Pd(II) complexes with condensation products of ethyl hydrazainoacetate and quinoline-8-carboxaldehyde (complex 1) and 2-for-mylpyridine (complex 3), for which apoptosis was determined as a mechanism of anticancer activity, further investigation revealed that they arrest the cell cycle in G0/G1 phase, induce generation of reactive oxygen species and inhibit Topoisomerase I in vitro. In silico studies corroborate experimental findings that these complexes show topoisomerase inhibition activity in the micromolar range and indicate binding to a DNA's minor groove as another potential target. Based on the results obtained by circular dichroism and fluorescence spectroscopy measurements, the most active complexes are suitable to be delivered to a blood stream via human serum albumin.
PB  - Elsevier Science Inc, New York
T2  - Journal of Inorganic Biochemistry
T1  - Pd(II) complexes with N-heteroaromatic hydrazone ligands: Anticancer activity, in silico and experimental target identification
VL  - 199
DO  - 10.1016/j.jinorgbio.2019.110758
ER  - 

@article{
author = "Bjelogrlić, Snežana K. and Todorović, Tamara R. and Kojić, Milan and Sencanski, Milan and Nikolić, Milan and Visnjevac, Aleksandar and Araskov, Jovana and Miljković, Marija and Muller, Christian D. and Filipović, Nenad R.",
year = "2019",
abstract = "Anticancer activity of Pd complexes 1-5 with bidentate N-heteroaromatic hydrazone ligands was investigated on human acute monocytic leukemia (THP-1; cells in a suspension) and human mammary adenocarcinoma (MCF-7; two-dimensional layer and three-dimensional spheroid tumor model) cell lines. For the Pd(II) complexes with condensation products of ethyl hydrazainoacetate and quinoline-8-carboxaldehyde (complex 1) and 2-for-mylpyridine (complex 3), for which apoptosis was determined as a mechanism of anticancer activity, further investigation revealed that they arrest the cell cycle in G0/G1 phase, induce generation of reactive oxygen species and inhibit Topoisomerase I in vitro. In silico studies corroborate experimental findings that these complexes show topoisomerase inhibition activity in the micromolar range and indicate binding to a DNA's minor groove as another potential target. Based on the results obtained by circular dichroism and fluorescence spectroscopy measurements, the most active complexes are suitable to be delivered to a blood stream via human serum albumin.",
publisher = "Elsevier Science Inc, New York",
journal = "Journal of Inorganic Biochemistry",
title = "Pd(II) complexes with N-heteroaromatic hydrazone ligands: Anticancer activity, in silico and experimental target identification",
volume = "199",
doi = "10.1016/j.jinorgbio.2019.110758"
}

Bjelogrlić, S. K., Todorović, T. R., Kojić, M., Sencanski, M., Nikolić, M., Visnjevac, A., Araskov, J., Miljković, M., Muller, C. D.,& Filipović, N. R.. (2019). Pd(II) complexes with N-heteroaromatic hydrazone ligands: Anticancer activity, in silico and experimental target identification. in Journal of Inorganic Biochemistry
Elsevier Science Inc, New York., 199.
https://doi.org/10.1016/j.jinorgbio.2019.110758

Bjelogrlić SK, Todorović TR, Kojić M, Sencanski M, Nikolić M, Visnjevac A, Araskov J, Miljković M, Muller CD, Filipović NR. Pd(II) complexes with N-heteroaromatic hydrazone ligands: Anticancer activity, in silico and experimental target identification. in Journal of Inorganic Biochemistry. 2019;199.
doi:10.1016/j.jinorgbio.2019.110758 .

Bjelogrlić, Snežana K., Todorović, Tamara R., Kojić, Milan, Sencanski, Milan, Nikolić, Milan, Visnjevac, Aleksandar, Araskov, Jovana, Miljković, Marija, Muller, Christian D., Filipović, Nenad R., "Pd(II) complexes with N-heteroaromatic hydrazone ligands: Anticancer activity, in silico and experimental target identification" in Journal of Inorganic Biochemistry, 199 (2019),
https://doi.org/10.1016/j.jinorgbio.2019.110758 . .