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Synthesis, chemical characterization, PARP inhibition, DNA binding and cellular uptake of novel ruthenium(II)-arene complexes bearing benzamide derivatives in human breast cancer cells
dc.creator | Pavlović, Marijana | |
dc.creator | Tadić, Ana | |
dc.creator | Gligorijević, Nevenka | |
dc.creator | Poljarević, Jelena | |
dc.creator | Petrović, Tamara G. | |
dc.creator | Dojčinović, Biljana | |
dc.creator | Savić, Aleksandar | |
dc.creator | Radulović, Siniša | |
dc.date.accessioned | 2020-08-26T10:32:40Z | |
dc.date.available | 2020-08-26T10:32:40Z | |
dc.date.issued | 2020 | |
dc.identifier.issn | 0162-0134 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/3634 | |
dc.description.abstract | Inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) showed remarkable clinical efficacy in BRCA-mutated tumors. Based on the rational drug design, derivatives of PARP inhibitor 3-aminobenzamide (3-AB), 2-amino-4-methylbenzamide (L1) and 3-amino-N-methylbenzamide (L2), were coordinated to the ruthenium(II) ion, to form potential drugs affecting DNA and inhibiting PARP enzyme. The four conjugated complexes of formula: C1 [(ƞ6-toluene)Ru(L1)Cl]PF6, C2 [(ƞ6-p-cymene)Ru(L1)Cl]PF6, C3 [(ƞ6-toluene)Ru(L2)Cl2] and C4 [(ƞ6-p-cymene)Ru(L2)Cl2], have been synthesized and characterized. Colorimetric 3-(4.5-dimethylthiazol-2-yl)-2.5-diphenyltetrazolium bromide (MTT) assay showed the highest antiproliferative activity of C1 in HCC1937, MDA-MB-231, and MCF-7 breast cancer cells. Efficiency of inhibition of PARP-1 enzymatic activity in vitro decreased in order: C2 > C4 > 3-AB>C1 > C3. ICP-MS study of intracellular accumulation and distribution in BRCA1-mutated HCC1937 revealed that C1-C4 entered cells within 24 h. The complex C1 showed the highest intracellular accumulation, nuclear-targeting properties, and exhibited the highest DNA binding (39.2 ± 0.6 pg of Ru per μg of DNA) that resulted in the cell cycle arrest in the S phase. | en |
dc.language.iso | en | sr |
dc.publisher | Elsevier | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200168/RS// | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200043/RS// | sr |
dc.rights | restrictedAccess | sr |
dc.source | Journal of Inorganic Biochemistry | sr |
dc.subject | Antitumor agents | sr |
dc.subject | Breast cancer | sr |
dc.subject | PARP inhibitor | sr |
dc.subject | Ruthenium(II) | sr |
dc.title | Synthesis, chemical characterization, PARP inhibition, DNA binding and cellular uptake of novel ruthenium(II)-arene complexes bearing benzamide derivatives in human breast cancer cells | en |
dc.type | article | sr |
dc.rights.license | ARR | sr |
dcterms.abstract | Савић, Aлександар; Дојчиновић, Биљана; Петровић, Тамара; Пољаревић, Јелена; Радуловић, Синиша; Тадић, Aна; Павловић, Маријана; Глигоријевић, Невенка; | |
dc.rights.holder | Elsevier | sr |
dc.citation.volume | 210 | |
dc.citation.spage | 111155 | |
dc.citation.rank | M21~ | |
dc.description.other | The peer-reviewed version: [https://cer.ihtm.bg.ac.rs/handle/123456789/3713] | |
dc.identifier.pmid | 32768729 | |
dc.identifier.doi | 10.1016/j.jinorgbio.2020.111155 | |
dc.identifier.scopus | 2-s2.0-85088982547 | |
dc.identifier.wos | 000564739400016 | |
dc.type.version | publishedVersion | sr |