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dc.creatorSelaković, Života
dc.creatorOpsenica, Dejan
dc.creatorEaton, Brett
dc.creatorRetterer, Cary
dc.creatorBavari, Sina
dc.creatorBurnett, James C.
dc.creatorŠolaja, Bogdan
dc.creatorPanchal, Rekha G.
dc.date.accessioned2019-01-30T17:32:41Z
dc.date.available2019-01-30T17:32:41Z
dc.date.issued2012
dc.identifier.issn1999-4915
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/1109
dc.description.abstractEbola (EBOV) and Marburg (MARV) filoviruses are highly infectious pathogens causing deadly hemorrhagic fever in humans and non-human primates. Promising vaccine candidates providing immunity against filoviruses have been reported. However, the sporadic nature and swift progression of filovirus disease underlines the need for the development of small molecule therapeutics providing immediate antiviral effects. Herein we describe a brief structural exploration of two previously reported diazachrysene (DAAC)-based EBOV inhibitors. Specifically, three analogs were prepared to examine how slight substituent modifications would affect inhibitory efficacy and inhibitor-mediated toxicity during not only EBOV, but also MARV cellular infection. Of the three analogs, one was highly efficacious, providing IC50 values of 0.696 mu M +/- 0.13 mu M and 2.76 mu M +/- 0.21 mu M against EBOV and MARV infection, respectively, with little or no associated cellular toxicity. Overall, the structure-activity and structure-toxicity results from this study provide a framework for the future development of DAAC-based filovirus inhibitors that will be both active and non-toxic in vivo.en
dc.publisherMdpi Ag, Basel
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS//
dc.relationFrederick National Laboratory for Cancer Research, National Institutes of Health (US) [HHSN261200800001E]
dc.relationJoint Science and Technology Office [TMTI_00048_RD_T]
dc.rightsopenAccess
dc.sourceViruses-Basel
dc.subjectfilovirusen
dc.subjectEbola virusen
dc.subjectMarburg virusen
dc.subjectantiviralen
dc.subjectdiazachryseneen
dc.subjectinhibitory efficacyen
dc.subjecttoxicityen
dc.subjectsmall moleculeen
dc.titleA Limited Structural Modification Results in a Significantly More Efficacious Diazachrysene-Based Filovirus Inhibitoren
dc.typearticle
dc.rights.licenseBY
dcterms.abstractОпсеница, Дејан; Реттерер, Царy; Еатон, Бретт; Солаја, Богдан A.; Бавари, Сина; Бурнетт, Јамес Ц.; Панцхал, Рекха Г.; Селаковиц, Зивота;
dc.citation.volume4
dc.citation.issue8
dc.citation.spage1279
dc.citation.epage1288
dc.citation.other4(8): 1279-1288
dc.citation.rankM22
dc.identifier.pmid23012625
dc.identifier.doi10.3390/v4081279
dc.identifier.rcubConv_2840
dc.identifier.fulltexthttp://cer.ihtm.bg.ac.rs//bitstream/id/7653/1107.pdf
dc.identifier.scopus2-s2.0-84868605426
dc.identifier.wos000308213000007
dc.type.versionpublishedVersion


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