| Yazarlar |
Hasan Yakan
Ondokuz Mayıs Üniversitesi, Türkiye |
|
Mohammed Azam
|
|
Sevgi Kansız
Türkiye |
Doç. Dr. Halit MUĞLU
Kastamonu Üniversitesi, Türkiye |
|
Mustafa Ergül
Türkiye |
|
Parham Taslımı
Bartın Üniversitesi, Türkiye |
|
Ümit Muhammet Koçyiğit
Türkiye |
|
Muhammet Karaman
Türkiye |
|
Saud I. Al-Resayes
|
|
Kim Min
|
| Özet |
| We are reporting a novel series of thiosemicarbazone derivatives derived from isatin (1-6), structural determination, and investigation of the inhibitory properties against proliferative, carbonic anhydrase, and cholinesterase enzymes. The anti-proliferative effects of the compounds were measured by XTT assay against MCF- 7 and MDA-MB-231 cancerous cell lines. Compound 3 showed significant cytotoxic effects on both MCF-7 and MDA-MB-231 cell lines, with IC50 values of 8.19 μM and 23.41 μM, respectively. In addition, the compounds (1- 6) inhibited the hCA I and II, their Ki values 2.01 ± 0.35 - 21.55 ± 2.56 and 1.24 ± 0.33 - 25.03 ± 5.48 μM, respectively. AChE was also successfully inhibited by these compounds (1-6), with Ki values ranging from 40.37 ± 8.23 to 125.43 ± 24.93 μM. The best Ki values for 3, 6, and 4 for α-glycosidase were 564.35 ± 72.06, 594.38 ± 52.04, and 683.437 ± 66.58 μM, respectively. Binding affinities were determined to be -6.697 kcal/mol, -8.251 kcal/mol, -9.932 kcal/mol, and -4.946 kcal/mol for hCA I, hCA II, AChE, and α-glucosidase enzymes, respectively. These findings reveal that the formed compounds containing isatin moieties were crucial in the enzyme inhibition. |
| Anahtar Kelimeler |
| Anti-proliferative activity | Enzyme inhibition | Isatin | Molecular docking | Thiosemicarbazone |
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale |
| Dergi Adı | Bulletin of the Chemical Society of Ethiopia |
| Dergi ISSN | 1011-3924 |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q3 |
| Makale Dili | İngilizce |
| Basım Tarihi | 04-2023 |
| Cilt No | 37 |
| Sayı | 5 |
| Sayfalar | 1221 / 1236 |
| Doi Numarası | 10.4314/bcse.v37i5.14 |
| Makale Linki | https://www.ajol.info/index.php/bcse/article/view/250487 |
| Atıf Sayıları | |
| SCOPUS | 6 |
