Novel thiazolidinedione hybrids as cholinesterase inhibitors and targeting neuroblastoma: design, synthesis, in vitro and in silico biological evaluations
Yazarlar (5)
Dr. Öğr. Üyesi Gurbet Çelik Turgut Pamukkale Üniversitesi, Türkiye
Arş. Gör. Furkan Çakır Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Prof. Dr. Alaattin Şen Pamukkale Üniversitesi, Türkiye
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Bioorganic Chemistry (Q1) | ||
| Dergi ISSN | 0045-2068 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 09-2025 |
| Cilt / Sayı / Sayfa | 164 / 1 / 108869–0 | DOI | 10.1016/j.bioorg.2025.108869 |
| Makale Linki | https://doi.org/10.1016/j.bioorg.2025.108869 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| In this study, a novel series of eleven 3,5-disubstituted thiazolidine-2,4-dione (TZD) derivatives were rationally designed and synthesized, incorporating tertiary amine moieties to enhance cholinesterase binding. The acetamide-linked TZD scaffold was selected for its potential dual functionality: cholinesterase inhibition and cytotoxicity against neuronal cells. All compounds were evaluated for their inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), alongside cytotoxicity assays on SH-SY5Y cancerous neuroblastoma and HEK-293 healthy cells. Compound 7 showed the strongest AChE inhibition (IC50 = 17.87 μM and Ki = 19.48 μM), while compound 8 exhibited the most potent BChE inhibition (IC50 = 34.98 μM and Ki = 26.15 μM), showing better activity than reference inhibitors (IC50Tacrine = 53.81 μM and IC50Galantamine = 43.21 μM). Several … |
| Anahtar Kelimeler |
| AChE | BChE | Cholinesterase inhibition | Neurodegenerative disorders | SH-SY5Y |
Science Direct
Novel thiazolidinedione hybrids as cholinesterase inhibitors and targeting neuroblastoma: design, synthesis, in vitro and in silico biological evaluations
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 12 |
| Scopus | 12 |
| Google Scholar | 11 |