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dc.creatorPavlović, Marijana
dc.creatorTadić, Ana
dc.creatorGligorijević, Nevenka
dc.creatorPoljarević, Jelena
dc.creatorPetrović, Tamara G.
dc.creatorDojčinović, Biljana
dc.creatorSavić, Aleksandar
dc.creatorRadulović, Siniša
dc.date.accessioned2020-08-26T10:32:40Z
dc.date.available2020-08-26T10:32:40Z
dc.date.issued2020
dc.identifier.issn0162-0134
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/3634
dc.description.abstractInhibitors 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.isoensr
dc.publisherElseviersr
dc.relationinfo:eu-repo/grantAgreement/MESTD/inst-2020/200168/RS//sr
dc.relationinfo:eu-repo/grantAgreement/MESTD/inst-2020/200043/RS//sr
dc.rightsrestrictedAccesssr
dc.sourceJournal of Inorganic Biochemistrysr
dc.subjectAntitumor agentssr
dc.subjectBreast cancersr
dc.subjectPARP inhibitorsr
dc.subjectRuthenium(II)sr
dc.titleSynthesis, chemical characterization, PARP inhibition, DNA binding and cellular uptake of novel ruthenium(II)-arene complexes bearing benzamide derivatives in human breast cancer cellsen
dc.typearticlesr
dc.rights.licenseARRsr
dcterms.abstractСавић, Aлександар; Дојчиновић, Биљана; Петровић, Тамара; Пољаревић, Јелена; Радуловић, Синиша; Тадић, Aна; Павловић, Маријана; Глигоријевић, Невенка;
dc.rights.holderElseviersr
dc.citation.volume210
dc.citation.spage111155
dc.citation.rankM21~
dc.description.otherThe peer-reviewed version: [https://cer.ihtm.bg.ac.rs/handle/123456789/3713]
dc.identifier.pmid32768729
dc.identifier.doi10.1016/j.jinorgbio.2020.111155
dc.identifier.scopus2-s2.0-85088982547
dc.identifier.wos000564739400016
dc.type.versionpublishedVersionsr


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