Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles
Yazarlar (8)
Cumhuriyet Üniversitesi, Türkiye
Prof. Dr. Yakup BUDAK
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Meliha Burcu GÜRDERE
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
İstanbul Arel Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
Prof. Dr. Mustafa CEYLAN
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | Archives of Physiology and Biochemistry |
| Dergi ISSN | 1381-3455 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q4 |
| Makale Dili | İngilizce |
| Basım Tarihi | 01-2018 |
| Cilt No | 124 |
| Sayı | 1 |
| Sayfalar | 61 / 68 |
| DOI Numarası | 10.1080/13813455.2017.1360914 |
| Makale Linki | https://www.tandfonline.com/doi/full/10.1080/13813455.2017.1360914 |
| Özet |
| 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 IC values in the range of 7.06-67.46 μM. IC value of 5-fluorouracil (5-FU) was 90.36 μM. Moreover, most of compounds 5a-g showed high antibacterial activity with 8-20 mm of inhibition zone (19-25 mm 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 70.470-229.42 nM against AChE. On the other hand, acetazolamide, clinically used drug, showed a Ki value of 977.77 ± 227.4 nM 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. |
| Anahtar Kelimeler |
| Chalcone-imide | acetylcholinesterase | anticancer activity | antimicrobial activity | carbonic anhydrase |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| WoS | 136 |
| Google Scholar | 170 |