Please use this identifier to cite or link to this item:
https://open.uns.ac.rs/handle/123456789/19207
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Petronijević Jelena | en_US |
dc.contributor.author | Janković Nenad | en_US |
dc.contributor.author | Stanojković Tatjana P. | en_US |
dc.contributor.author | Joksimović Nenad | en_US |
dc.contributor.author | Grozdanić Nađa | en_US |
dc.contributor.author | Vraneš Milan | en_US |
dc.contributor.author | Aleksandar Tot | en_US |
dc.contributor.author | Bugarčić Zorica | en_US |
dc.date.accessioned | 2020-12-13T13:29:35Z | - |
dc.date.available | 2020-12-13T13:29:35Z | - |
dc.date.issued | 2018 | - |
dc.identifier.issn | 0365-6233 | en_US |
dc.identifier.uri | https://open.uns.ac.rs/handle/123456789/19207 | - |
dc.description.abstract | © 2018 Deutsche Pharmazeutische Gesellschaft In order to investigate new potential therapeutically active agents, we investigated the biological properties of two small libraries of quinoxalinones and 1,4-benzoxazin-2-ones. The results obtained showed that compounds 5, 9–11 have good cytotoxic activity against HeLa cells where the lowest IC50value (10.46 ± 0.82 μM/mL) was measured for compound 10. Additionally, the most active compounds (5, 9–11) showed much better selectivity for MRC-5 cells (up to 17.4) compared to cisplatin. In vitro evaluation of the inhibition of the enzyme α-glucosidase showed that compounds 10 and 11 exert significant inhibition of the enzyme at 52.54 ± 0.09 and 40.09 ± 0.49 μM, respectively. Competitive experiments with ethidium bromide (EB) indicated that all tested compounds have affinity to displace EB from the EB-DNA complex through intercalation, suggesting good competition with EB (Ksv= (3.1 ± 0.2), (5.1 ± 0.1), (5.6 ± 0.2), and (6.3 ± 0.2) × 103M−1). A molecular docking study was also performed to better understand the binding modes and to conclude the structure–activity relationships of the synthesized compounds. | - |
dc.language.iso | en | en_US |
dc.relation.ispartof | Archiv der Pharmazie | - |
dc.source | CRIS UNS | - |
dc.source.uri | http://cris.uns.ac.rs | - |
dc.title | Biological evaluation of selected 3,4-dihydro-2(1H)-quinoxalinones and 3,4-dihydro-1,4-benzoxazin-2-ones: Molecular docking study | en_US |
dc.type | Journal/Magazine Article | en_US |
dc.identifier.doi | 10.1002/ardp.201700308 | - |
dc.identifier.doi | (BISIS)109428 | - |
dc.identifier.pmid | 351 | - |
dc.identifier.scopus | 85045481725 | - |
dc.identifier.url | https://www.cris.uns.ac.rs/record.jsf?recordId=109428&source=BEOPEN&language=en | - |
dc.identifier.url | https://api.elsevier.com/content/abstract/scopus_id/85045481725 | - |
dc.description.version | Unknown | en_US |
dc.relation.issue | 5 | - |
dc.relation.volume | 351 | - |
dc.identifier.externalcrisreference | (BISIS)109428 | - |
item.fulltext | No Fulltext | - |
item.grantfulltext | none | - |
crisitem.author.dept | Departman za hemiju, biohemiju i zaštitu životne sredine | - |
crisitem.author.dept | Departman za hemiju, biohemiju i zaštitu životne sredine | - |
crisitem.author.parentorg | Prirodno-matematički fakultet | - |
crisitem.author.parentorg | Prirodno-matematički fakultet | - |
Appears in Collections: | PMF Publikacije/Publications |
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