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dc.contributor.authorKoçyiğit, Ümit Muhammet
dc.contributor.authorBudak, Yakup
dc.contributor.authorGürdere, Meliha Burcu
dc.contributor.authorErturk, Fatih
dc.contributor.authorYençilek, Belkız
dc.contributor.authorTaslimi, Parham
dc.contributor.authorGülçin, İlhami
dc.contributor.authorCeylan, Mustafa
dc.date.accessioned2019-05-29T10:24:49Z
dc.date.available2019-05-29T10:24:49Z
dc.date.issued2018
dc.identifier.citationKocyigit, U. M., Budak, Y., Gurdere, M. B., Erturk, F., Yencilek, B., Taslimi, P., . . . Ceylan, M. (2018). Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles. Archives of Physiology and Biochemistry, 124(1), 61-68.en_US
dc.identifier.issn1381-3455
dc.identifier.issn1744-4160
dc.identifier.urihttps://hdl.handle.net/20.500.12294/1423
dc.descriptionErtürk, Fatih (Arel Author)en_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.language.isoengen_US
dc.publisherTaylor & Francisen_US
dc.relation.isversionof10.1080/13813455.2017.1360914en_US
dc.rightsinfo:eu-repo/semantics/openAccessen_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.identifier.volume124en_US
dc.identifier.issue1en_US
dc.identifier.startpage61en_US
dc.identifier.endpage68en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.relation.tubitakinfo:eu-repo/grantAgreement/TUBITAK/SOBAG/111T990


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