dc.contributor.author | Kocyigit, Umit Muhammet | |
dc.contributor.author | Budak, Yakup | |
dc.contributor.author | Gurdere, Meliha Burcu | |
dc.contributor.author | Erturk, Fatih | |
dc.contributor.author | Yencilek, Belkiz | |
dc.contributor.author | Taslimi, Parham | |
dc.contributor.author | Gulcin, Ilhami | |
dc.contributor.author | Ceylan, Mustafa | |
dc.date.accessioned | 2019-07-27T12:10:23Z | |
dc.date.accessioned | 2019-07-28T09:38:55Z | |
dc.date.available | 2019-07-27T12:10:23Z | |
dc.date.available | 2019-07-28T09:38:55Z | |
dc.date.issued | 2018 | |
dc.identifier.issn | 1381-3455 | |
dc.identifier.issn | 1744-4160 | |
dc.identifier.uri | https://dx.doi.org/10.1080/13813455.2017.1360914 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/6439 | |
dc.description | WOS: 000425063500008 | en_US |
dc.description | PubMed ID: 28792233 | en_US |
dc.description.abstract | The 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.sponsorship | Scientific and Technological Research Council of Turkey [TUBITAK Project] [111T990] | en_US |
dc.description.sponsorship | The authors are indebted to the Scientific and Technological Research Council of Turkey [TUBITAK Project No. 111T990] for financial supports. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | TAYLOR & FRANCIS LTD | en_US |
dc.relation.isversionof | 10.1080/13813455.2017.1360914 | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Chalcone-imide | en_US |
dc.subject | anticancer activity | en_US |
dc.subject | antimicrobial activity | en_US |
dc.subject | acetylcholinesterase | en_US |
dc.subject | carbonic anhydrase | en_US |
dc.title | Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles | en_US |
dc.type | article | en_US |
dc.relation.journal | ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY | en_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, Turkey | en_US |
dc.contributor.authorID | GULCIN, Ilhami -- 0000-0001-5993-1668 | en_US |
dc.identifier.volume | 124 | en_US |
dc.identifier.issue | 1 | en_US |
dc.identifier.endpage | 68 | en_US |
dc.identifier.startpage | 61 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |