dc.contributor.author | Hasan Yakan | |
dc.contributor.author | Mohammed Azam | |
dc.contributor.author | Sevgi Kansız | |
dc.contributor.author | Halit Muğlu | |
dc.contributor.author | Mustafa Ergül | |
dc.contributor.author | Parham Taslimi | |
dc.contributor.author | Ümit M Koçyiğit | |
dc.contributor.author | Muhammet Karaman | |
dc.contributor.author | Saud I Al-Resayes | |
dc.contributor.author | Kim Min | |
dc.date.accessioned | 2024-03-07T07:52:51Z | |
dc.date.available | 2024-03-07T07:52:51Z | |
dc.date.issued | 2023/7/3 | tr |
dc.identifier.citation | APA | tr |
dc.identifier.uri | https://www.ajol.info/index.php/bcse/article/view/250487 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/14847 | |
dc.description | . | tr |
dc.description.abstract | 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. | tr |
dc.description.sponsorship | This work was supported by Scientific Research Project Fund of Sivas Cumhuriyet University
(Project number SHMYO-013). The authors acknowledge the financial support through
Researchers Supporting Project number (RSP2023R147), King Saud University, Riyadh, Saudi
Arabia. | tr |
dc.language.iso | eng | tr |
dc.publisher | AJOL | tr |
dc.relation.isversionof | https://dx.doi.org/10.4314/bcse.v37i5.14 | tr |
dc.rights | info:eu-repo/semantics/closedAccess | tr |
dc.subject | Isatin, Thiosemicarbazone, Anti-proliferative activity, Enzyme inhibition, Molecular docking | tr |
dc.title | Isatin/thiosemicarbohydrazone hybrids: Facile synthesis, and their evaluation as anti-proliferatıve agents and metabolıc enzyme inhibitors | tr |
dc.title.alternative | . | tr |
dc.type | article | tr |
dc.relation.journal | Bulletin of the Chemical Society of Ethiopia | tr |
dc.contributor.department | Eczacılık Fakültesi | tr |
dc.contributor.authorID | https://orcid.org/0000-0001-8710-2912 | tr |
dc.identifier.volume | 37 | tr |
dc.identifier.issue | 5 | tr |
dc.identifier.endpage | 1236 | tr |
dc.identifier.startpage | 1221 | tr |
dc.relation.publicationcategory | Uluslararası Hakemli Dergide Makale - Kurum Öğretim Elemanı | tr |