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dc.creatorPavić, Aleksandar
dc.creatorGlisic, Biljana D.
dc.creatorVojnovic, Sandra
dc.creatorWarzajtis, Beata
dc.creatorSavic, Nada D.
dc.creatorAntic, Marija
dc.creatorRadenković, Slavko
dc.creatorJanjić, Goran
dc.creatorNikodinović-Runić, Jasmina
dc.creatorRychlewska, Urszula
dc.creatorĐuran, Miloš
dc.date.accessioned2019-01-30T17:54:13Z
dc.date.available2019-01-30T17:54:13Z
dc.date.issued2017
dc.identifier.issn0162-0134
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2136
dc.description.abstractGold(III) complexes with 1,7- and 4,7-phenanthroline ligands, [AuCl3(1,7-phen-kappa N7)] (1) and [AuCl3(4,7-phen-kappa N4)] (2) were synthesized and structurally characterized by spectroscopic (NMR, IR and UV-vis) and single crystal X-ray diffraction techniques. In these complexes, 1,7- and 4,7-phenanthrolines are monodentatedly coordinated to the Au(III) ion through the N7 and N4 nitrogen atoms, respectively. In comparison to the clinically relevant anti-angiogenic compounds auranofin and sunitinib, gold(III)-phenanthroline complexes showed from 1.5- to 20-fold higher anti-angiogenic potential, and 13- and 118-fold lower toxicity. Among the tested compounds, complex 1 was the most potent and may be an excellent anti-angiogenic drug candidate, since it showed strong anti-angiogenic activity in zebrafish embryos achieving IC50 value (concentration resulting in an anti-angiogenic phenotype at 50% of embryos) of 2.89 mu M, while had low toxicity with LC50 value (the concentration inducing the lethal effect of 50% embryos) of 128 mu M. Molecular docking study revealed that both complexes and ligands could suppress angiogenesis targeting the multiple major regulators of angiogenesis, such as the vascular endothelial growth factor receptor (VEGFR-2), the matrix metalloproteases (MMP-2 and MMP-9), and thioredoxin reductase (TrxR1), where the complexes showed higher binding affinity in comparison to ligands, and particularly to auranofin, but comparable to sunitinib, an anti-angiogenic drug of clinical relevance.en
dc.publisherElsevier Science Inc, New York
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172036/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/173048/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/174033/RS//
dc.relationSupraMedChem"Balkans.Net SCOPES Institutional Partnership [IZ74Z0_160515]
dc.rightsrestrictedAccess
dc.sourceJournal of Inorganic Biochemistry
dc.subjectGold(III) complexesen
dc.subjectPhenanthrolineen
dc.subjectCytotoxicityen
dc.subjectEmbryotoxicityen
dc.subjectAngiogenesisen
dc.titleMononuclear gold(III) complexes with phenanthroline ligands as efficient inhibitors of angiogenesis: A comparative study with auranofin and sunitiniben
dc.typearticle
dc.rights.licenseARR
dcterms.abstractПавиц, Aлександар; Aнтиц, Марија; Раденковиц, Славко; Дјуран, Милос И.; Глисиц, Биљана Д.; Никодиновиц-Руниц, Јасмина; Рyцхлеwска, Урсзула; Савиц, Нада Д.; Wарзајтис, Беата; Јањић, Горан; Војновиц, Сандра;
dc.citation.volume174
dc.citation.spage156
dc.citation.epage168
dc.citation.other174: 156-168
dc.citation.rankM22
dc.description.otherThe peer-reviewed version: [http://cer.ihtm.bg.ac.rs/handle/123456789/2939]
dc.identifier.pmid28675847
dc.identifier.doi10.1016/j.jinorgbio.2017.06.009
dc.identifier.rcubConv_3762
dc.identifier.scopus2-s2.0-85021674718
dc.identifier.wos000406647700016
dc.type.versionpublishedVersion


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