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dc.creatorBondžić, Bojan
dc.creatorDžambaski, Zdravko
dc.creatorKolarević, Ana
dc.creatorĐorđević, Aleksandra
dc.creatorAnderluh, Marko
dc.creatorŠmelcerović, Andrija
dc.date.accessioned2020-12-03T11:55:35Z
dc.date.available2020-12-03T11:55:35Z
dc.date.issued2019
dc.identifier.issn1756-8919
dc.identifier.urihttps://cer.ihtm.bg.ac.rs/handle/123456789/3957
dc.description.abstractEight new benzocyclobutane-2,5-diones (1a–1h) were synthesized, and their inhibitory properties against bovine pancreatic DNase I were examined in vitro. Methods & results: Compounds 1a–1h were synthesized using photocycloaddition of duroquinone with various phenyl-substituted ethylenes in the presence of 18W compact fluorescent lamp (visible light). Two compounds, 1,3,4,6-tetramethyl-7- phenylbicyclo[4.2.0]oct-3-ene-2,5-dione (1a) and 1,3,4,6-tetramethyl-7-p-tolylbicyclo[4.2.0]oct-3-ene-2,5- dione (1b) inhibited DNase I in a noncompetitive manner with IC50 values below 150 μM and showed to be more potent DNase I inhibitors than crystal violet, used as a positive control. In order to analyze potential binding sites for the studied compounds with DNase I, molecular docking study was performed. Conclusion: The studied benzocyclobutane-2,5-diones offer a good starting point for a design of new DNase I inhibitors.en
dc.language.isoensr
dc.publisherFuture Medicine Ltd.sr
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172020/RS//sr
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172044/RS//sr
dc.relationFaculty of Medicine of the University of Nis (internal project no. 4)sr
dc.relationSlovenian Research Agency (grant no. P1-0208)sr
dc.rightsrestrictedAccesssr
dc.sourceFuture Medicinal Chemistrysr
dc.subjectbenzocyclobutane-2,5-dionessr
dc.subjectDNase I inhibitionsr
dc.subjectLineweaver–Burk plotsr
dc.subjectmolecular dockingsr
dc.subjectsynthesissr
dc.titleSynthesis and DNase I inhibitory properties of new benzocyclobutane-2,5-dionesen
dc.typearticlesr
dc.rights.licenseARRsr
dcterms.abstractКоларевић, Aна; Ђорђевић, Aлександра; Aндерлух, Марко; Джамбаски, Здравко; Бонджић, Бојан; Шмелцеровић, Aндрија;
dc.rights.holderNewlands Presssr
dc.citation.volume11
dc.citation.volume2426
dc.citation.issue18
dc.citation.spage2415
dc.citation.rankM22
dc.identifier.pmid31526044
dc.identifier.doi10.4155/fmc-2019-0032
dc.identifier.scopus2-s2.0-85072993481
dc.identifier.wos000498836900006
dc.type.versionpublishedVersionsr


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