Synthesis and investigation of anticancer, antibacterial activities and carbonic anhydrase, acetylcholinesterase inhibition profiles of novel (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones
Yazarlar (7)
Sivas Cumhuriyet Üniversitesi, Türkiye
Prof. Dr. Yakup BUDAK
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Meliha Burcu GÜRDERE
Tokat Gaziosmanpaşa 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 | Monatshefte für Chemie - Chemical Monthly |
| Dergi ISSN | 0026-9247 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Makale Dili | İngilizce |
| Basım Tarihi | 04-2019 |
| Cilt No | 150 |
| Sayı | 4 |
| Sayfalar | 721 / 731 |
| DOI Numarası | 10.1007/s00706-019-2350-z |
| Makale Linki | http://link.springer.com/10.1007/s00706-019-2350-z |
| Özet |
| Abstract A series of novel 1,3,5-trisubstituted pyrazoline derivatives, (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones, were synthesized and evaluated for their antimicrobial and anticancer activities. In addition, the compounds were tested against acetylcholinesterase (AChE) enzyme and two physiologically relevant carbonic anhydrase I and II isozymes (hCA I and II). In this study, inhibition of hCA I and hCA II by the novel synthesized 1,3,5-trisubstituted pyrazolines was impressive, with Ki values in the range of 3.33–7.90 nM for hCA I and 2.07–8.47 nM for hCA II, while the Ki values of these compounds for AChE were recorded in the range of 9.61–48.42 nM, respectively. Two compounds can be investigated as the leader compounds because of their lowest Ki values to make further detailed CA … |
| Anahtar Kelimeler |
| Bioorganic chemistry | Heterocyclics | Enzyme inhibition | Chalcone | Antimicrobial | Anticancer |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| WoS | 37 |
| Google Scholar | 44 |