ISATIN/THIOSEMICARBAZONE HYBRIDS: FACILE SYNTHESIS, AND THEIR EVALUATION AS ANTI-PROLIFERATIVE AGENTS AND METABOLIC ENZYME INHIBITORS
Yazarlar (10)
Hasan Yakan Ondokuz Mayis Üniversitesi, Türkiye
Mohammed Azam College Of Sciences, Suudi Arabistan
Dr. Öğr. Üyesi Sevgi Kansiz Samsun University, Türkiye
Prof. Dr. Halit MUĞLU Kastamonu Üniversitesi, Türkiye
Doç. Dr. Mustafa Ergül Cumhuriyet Üniversitesi, Türkiye
Doç. Dr. Parham Taslimi Bartin Üniversitesi, Türkiye
Ümit M. Koçyiǧit Cumhuriyet Üniversitesi, Türkiye
Doç. Dr. Muhammet Karaman Kilis 7 Aralik Üniversitesi, Türkiye
Saud I. Al-Resayes College Of Sciences, Suudi Arabistan
Kim Min
Dongguk University, Gyeongju, Güney Kore
Dongguk University, Gyeongju, Güney Kore
| Makale Türü |
Özgün Makale
(SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
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| Dergi Adı | Bulletin of the Chemical Society of Ethiopia (Q3) | ||
| Dergi ISSN | 1011-3924 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 06-2023 |
| Cilt / Sayı / Sayfa | 37 / 5 / 1221–1236 | DOI | 10.4314/bcse.v37i5.14 |
| Makale Linki | https://www.ajol.info/index.php/bcse/article/view/250487 | ||
| 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 |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Scopus | 15 |