Show simple item record

dc.creatorPopović-Đorđević, Jelena B.
dc.creatorJevtić, Ivana
dc.creatorGrozdanic, Nadja Dj
dc.creatorŠegan, Sandra
dc.creatorZlatović, Mario
dc.creatorIvanović, Milovan D.
dc.creatorStanojković, Tatjana
dc.date.accessioned2019-01-30T17:52:43Z
dc.date.available2019-01-30T17:52:43Z
dc.date.issued2017
dc.identifier.issn1475-6366
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2063
dc.description.abstractThe inhibitory activities of selected cyclic urea and carbamate derivatives (1-13) toward alpha-glucosidase (alpha-Gls) in in vitro assay were examined in this study. All examined compounds showed higher inhibitory activity (IC50) against alpha-Gls compared to standard antidiabetic drug acarbose. The most potent was benzyl (3,4,5-trimethoxyphenyl) carbamate (12) with IC50 = 49.85 +/- 0.10 mu M. In vitro cytotoxicity of the investigated compounds was tested on three human cancer cell lines HeLa, A549 and MDA-MB-453 using MTT assay. The best antitumour activity was achieved with compound 2 (trans-5-phenethyl-1-phenylhexahydro-1H-imidazo[4,5-c] pyridin-2(3H)-one) against MDA-MB-453 human breast cancer cell line (IC50 = 83.41 +/- 1.60 mu M). Cyclic ureas and carbamates showed promising anti-alpha-glucosidase activity and should be further tested as potential antidiabetic drugs. The PLS model of preliminary QSAR study indicated that, in planing the future synthesis of more potent compounds, the newly designed should have the substituents capable of polar interactions with receptor sites in various positions, while avoiding the increase of their lipophilicity.en
dc.publisherTaylor & Francis Ltd, Abingdon
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172032/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172055/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/175011/RS//
dc.rightsopenAccess
dc.rights.urihttps://creativecommons.org/licenses/by-nc/4.0/
dc.sourceJournal of Enzyme Inhibition and Medicinal Chemistry
dc.subjectalpha-Glucosidase inhibitorsen
dc.subjectcarbamatesen
dc.subjectcyclic ureasen
dc.subjectcytotoxicityen
dc.subjectQSARen
dc.titlealpha-Glucosidase inhibitory activity and cytotoxic effects of some cyclic urea and carbamate derivativesen
dc.typearticle
dc.rights.licenseBY-NC
dcterms.abstractПоповић-Ђорђевић, Јелена Б.; Јевтић, Ивана; Грозданиц, Надја Дј; Ивановиц, Милован Д.; Станојковиц, Татјана П.; Златовиц, Марио В.; Шеган, Сандра;
dc.citation.volume32
dc.citation.issue1
dc.citation.spage298
dc.citation.epage303
dc.citation.other32(1): 298-303
dc.citation.rankaM21
dc.identifier.pmid28100083
dc.identifier.doi10.1080/14756366.2016.1250754
dc.identifier.rcubConv_3662
dc.identifier.fulltexthttp://cer.ihtm.bg.ac.rs//bitstream/id/8493/2061.pdf
dc.identifier.scopus2-s2.0-85013757766
dc.identifier.wos000392591100024
dc.type.versionpublishedVersion


Files in this item

Thumbnail

This item appears in the following Collection(s)

Show simple item record