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Pd(II) complexes with N-heteroaromatic hydrazone ligands: Anticancer activity, in silico and experimental target identification
dc.creator | Bjelogrlić, Snežana | |
dc.creator | Todorović, Tamara R. | |
dc.creator | Kojić, Milan | |
dc.creator | Sencanski, Milan | |
dc.creator | Nikolić, Milan | |
dc.creator | Visnjevac, Aleksandar | |
dc.creator | Araskov, Jovana | |
dc.creator | Miljković, Marija | |
dc.creator | Muller, Christian D. | |
dc.creator | Filipović, Nenad | |
dc.date.accessioned | 2020-12-17T22:29:07Z | |
dc.date.available | 2020-12-17T22:29:07Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 0162-0134 | |
dc.identifier.uri | http://aspace.agrif.bg.ac.rs/handle/123456789/4916 | |
dc.description.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. | en |
dc.publisher | Elsevier Science Inc, New York | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172055/RS// | |
dc.relation | COSTEuropean Cooperation in Science and Technology (COST) [CA15135, CA16119] | |
dc.rights | restrictedAccess | |
dc.source | Journal of Inorganic Biochemistry | |
dc.subject | Pd(II) complexes | en |
dc.subject | Hydrazones | en |
dc.subject | Apoptosis | en |
dc.subject | Topoisomerase I inhibition | en |
dc.subject | DNA interactions | en |
dc.subject | HSA interactions | en |
dc.title | Pd(II) complexes with N-heteroaromatic hydrazone ligands: Anticancer activity, in silico and experimental target identification | en |
dc.type | article | |
dc.rights.license | ARR | |
dc.citation.other | 199: - | |
dc.citation.rank | M21 | |
dc.citation.volume | 199 | |
dc.identifier.doi | 10.1016/j.jinorgbio.2019.110758 | |
dc.identifier.scopus | 2-s2.0-85068530825 | |
dc.identifier.pmid | 31299379 | |
dc.identifier.wos | 000488146900009 | |
dc.type.version | publishedVersion |