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dc.contributor.authorKocyigit, Umit Muhammet
dc.contributor.authorBudak, Yakup
dc.contributor.authorGurdere, Meliha Burcu
dc.contributor.authorErturk, Fatih
dc.contributor.authorYencilek, Belkiz
dc.contributor.authorTaslimi, Parham
dc.contributor.authorGulcin, Ilhami
dc.contributor.authorCeylan, Mustafa
dc.date.accessioned2019-07-27T12:10:23Z
dc.date.accessioned2019-07-28T09:38:55Z
dc.date.available2019-07-27T12:10:23Z
dc.date.available2019-07-28T09:38:55Z
dc.date.issued2018
dc.identifier.issn1381-3455
dc.identifier.issn1744-4160
dc.identifier.urihttps://dx.doi.org/10.1080/13813455.2017.1360914
dc.identifier.urihttps://hdl.handle.net/20.500.12418/6439
dc.descriptionWOS: 000425063500008en_US
dc.descriptionPubMed ID: 28792233en_US
dc.description.abstractThe new 1-(4-(3-(aryl)acryloyl)phenyl)-1H-pyrrole-2,5-diones (5a-g) were prepared from 4-aminchalcones (3a-g) and screened for biological activities. All compounds (3a-g and 5a-g), except 3d and 3e displayed good cytotoxic activities with IC50 values in the range of 7.06-67.46 mu M. IC50 value of 5-fluorouracil (5-FU) was 90.36 mu M. Moreover, most of compounds 5a-g showed high antibacterial activity with 8-20 mm of inhibition zone (19-25mm of Sulbactam-Cefoperazone (SCF)). In addition, they showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase I, and II (hCA I and hCA II) isoforms. Also, these compounds demonstrated effective inhibition profiles with Ki values of 426.47-699.58 nM against hCA I, 214.92-532.21 nM against hCA II, and 70.470-229.42nM against AChE. On the other hand, acetazolamide, clinically used drug, showed a Ki value of 977.77 +/- 227.4nM against CA I, and 904.47 +/- 106.3 nM against CA II, respectively. Also, tacrine inhibited AChE showed a Ki value of 446.56 +/- 58.33 nM.en_US
dc.description.sponsorshipScientific and Technological Research Council of Turkey [TUBITAK Project] [111T990]en_US
dc.description.sponsorshipThe authors are indebted to the Scientific and Technological Research Council of Turkey [TUBITAK Project No. 111T990] for financial supports.en_US
dc.language.isoengen_US
dc.publisherTAYLOR & FRANCIS LTDen_US
dc.relation.isversionof10.1080/13813455.2017.1360914en_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectChalcone-imideen_US
dc.subjectanticancer activityen_US
dc.subjectantimicrobial activityen_US
dc.subjectacetylcholinesteraseen_US
dc.subjectcarbonic anhydraseen_US
dc.titleSynthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profilesen_US
dc.typearticleen_US
dc.relation.journalARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRYen_US
dc.contributor.department[Kocyigit, Umit Muhammet] Cumhuriyet Univ, Vocat Sch Hlth Serv, Sivas, Turkey -- [Budak, Yakup -- Gurdere, Meliha Burcu -- Yencilek, Belkiz -- Ceylan, Mustafa] Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey -- [Erturk, Fatih] Istanbul Arel Univ, Vocat Sch, Occupat Hlth & Safety Programme, Istanbul, Turkey -- [Taslimi, Parham -- Gulcin, Ilhami] Ataturk Univ, Dept Chem, Fac Sci, TR-25240 Erzurum, Turkeyen_US
dc.contributor.authorIDGULCIN, Ilhami -- 0000-0001-5993-1668en_US
dc.identifier.volume124en_US
dc.identifier.issue1en_US
dc.identifier.endpage68en_US
dc.identifier.startpage61en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US


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