Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles
Yazarlar (8)
Ümit Muhammet Koçyiğit Cumhuriyet Üniversitesi, Türkiye
Prof. Dr. Yakup BUDAK Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Meliha Burcu GÜRDERE Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Fatih Ertürk İstanbul Arel Üniversitesi, Türkiye
Belkız Yencilek
İlhami Gülçin Atatürk Üniversitesi, Türkiye
Prof. Dr. Mustafa CEYLAN Tokat Gaziosmanpaşa Üniversitesi, Türkiye
| Makale Türü |
Özgün Makale
(SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
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| Dergi Adı | ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY (Q4) | ||
| Dergi ISSN | 1381-3455 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 01-2018 |
| Cilt / Sayı / Sayfa | 124 / 1 / 61–68 | DOI | 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 IC50 values in the range of 7.06–67.46 μM. IC50 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 … |
| Anahtar Kelimeler |
| Chalcone-imide | acetylcholinesterase | anticancer activity | antimicrobial activity | carbonic anhydrase |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Google Scholar | 170 |
| Web of Science | 137 |