dc.creator | Bondžić, Bojan | |
dc.creator | Džambaski, Zdravko | |
dc.creator | Kolarević, Ana | |
dc.creator | Đorđević, Aleksandra | |
dc.creator | Anderluh, Marko | |
dc.creator | Šmelcerović, Andrija | |
dc.date.accessioned | 2020-12-03T11:55:35Z | |
dc.date.available | 2020-12-03T11:55:35Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 1756-8919 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/3957 | |
dc.description.abstract | Eight 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.iso | en | sr |
dc.publisher | Future Medicine Ltd. | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172020/RS// | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172044/RS// | sr |
dc.relation | Faculty of Medicine of the University of Nis (internal project no. 4) | sr |
dc.relation | Slovenian Research Agency (grant no. P1-0208) | sr |
dc.rights | restrictedAccess | sr |
dc.source | Future Medicinal Chemistry | sr |
dc.subject | benzocyclobutane-2,5-diones | sr |
dc.subject | DNase I inhibition | sr |
dc.subject | Lineweaver–Burk plot | sr |
dc.subject | molecular docking | sr |
dc.subject | synthesis | sr |
dc.title | Synthesis and DNase I inhibitory properties of new benzocyclobutane-2,5-diones | en |
dc.type | article | sr |
dc.rights.license | ARR | sr |
dcterms.abstract | Коларевић, Aна; Ђорђевић, Aлександра; Aндерлух, Марко; Джамбаски, Здравко; Бонджић, Бојан; Шмелцеровић, Aндрија; | |
dc.rights.holder | Newlands Press | sr |
dc.citation.volume | 11 | |
dc.citation.volume | 2426 | |
dc.citation.issue | 18 | |
dc.citation.spage | 2415 | |
dc.citation.rank | M22 | |
dc.identifier.pmid | 31526044 | |
dc.identifier.doi | 10.4155/fmc-2019-0032 | |
dc.identifier.scopus | 2-s2.0-85072993481 | |
dc.identifier.wos | 000498836900006 | |
dc.type.version | publishedVersion | sr |