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Pd(II) complexes with N-heteroaromatic hydrazone ligands: Anticancer activity, in silico and experimental target identification
dc.creator | Bjelogrlić, Snežana K. | |
dc.creator | Todorović, Tamara | |
dc.creator | Kojić, Milan O. | |
dc.creator | Senćanski, Milan | |
dc.creator | Nikolić, Milan | |
dc.creator | Višnjevac, Aleksandar | |
dc.creator | Araškov, Jovana | |
dc.creator | Miljković, Marija | |
dc.creator | Muller, Christian D. | |
dc.creator | Filipović, Nenad R. | |
dc.date.accessioned | 2019-08-22T15:21:44Z | |
dc.date.available | 2019-08-22T15:21:44Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 0162-0134 | |
dc.identifier.uri | https://cherry.chem.bg.ac.rs/handle/123456789/3318 | |
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-formylpyridine (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. | |
dc.publisher | Elsevier | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172055/RS// | |
dc.relation | COST | |
dc.rights | restrictedAccess | |
dc.source | Journal of Inorganic Biochemistry | |
dc.subject | Apoptosis | |
dc.subject | DNA interactions | |
dc.subject | HSA interactions | |
dc.subject | Hydrazones | |
dc.subject | Pd(II) complexes | |
dc.subject | Topoisomerase I inhibition | |
dc.title | Pd(II) complexes with N-heteroaromatic hydrazone ligands: Anticancer activity, in silico and experimental target identification | |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Филиповић, Ненад Р.; Миљковић, Марија; Бјелогрлић, Снежана К.; Тодоровић, Тамара Р.; Којић, Милан О.; Сенћански, Милан; Николић, Милан; Вишњевац, Aлександар; Aрашков, Јована; Муллер, Цхристиан Д.; | |
dc.citation.volume | 199 | |
dc.identifier.wos | 000488146900009 | |
dc.identifier.doi | 10.1016/j.jinorgbio.2019.110758 | |
dc.citation.rank | M21~ | |
dc.description.other | Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3319] | |
dc.type.version | publishedVersion | |
dc.identifier.scopus | 2-s2.0-85068530825 |