Microwave-assisted synthesis of indanone-based mannich base derivatives: In Silico study, evaluations of dual enzyme inhibition, drug-likeness, cytotoxicity, and selectivity properties
Yazarlar (6)
Doç. Dr. Mehtap TUĞRAK SAKARYA Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Halise Inci Gul Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Hiroshi Sakagami
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Yusuf Sert Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Selma Sarac
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Ilhami Gulcin Tokat Gaziosmanpaşa Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Journal of Molecular Structure (Q2) | ||
| Dergi ISSN | 0022-2860 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 04-2026 |
| Cilt / Sayı / Sayfa | 1358 / 1 / 145363– | DOI | 10.1016/j.molstruc.2026.145363 |
| Makale Linki | https://doi.org/10.1016/j.molstruc.2026.145363 | ||
| Özet |
| In the present study, two series of mono Mannich bases (C1-C5 and CPM1-CPM5) were synthesized by reacting 2-(3-hydroxybenzylidene)-2,3-dihydro-1H-inden-1-one (C) with paraformaldehyde and secondary amines. Amine parts were replaced with N-methylpiperazine, morpholine, piperidine, pyrrolidine, dimethylamine, and substituted piperazines (C1-C5, CPM1-CPM5). In vitro cytotoxicity of the compounds was tested against oral cancer cell lines (Ca9-22, HSC-2) and normal oral cells (HGF, HPLF) using the MTT assay. According to potency selectivity expression (PSE) values, C5 (21.6) and CPM1 (19.2) showed the best selective cytotoxicity. All compounds exhibited significantly lower Ki values than the reference inhibitor acetazolamide (AZA), which showed Ki values of 183.39 ± 19.71 nM against hCA I and 104.60 ± 27.60 nM against hCA II, indicating superior inhibitory potency of the tested compounds … |
| Anahtar Kelimeler |
| Acetylcholine esterase | Carbonic anhydrase | Cytotoxicity | In silico | Indanone | Mannich bases | Tumour selectivity |
Science Direct
Microwave-assisted synthesis of indanone-based mannich base derivatives: In Silico study, evaluations of dual enzyme inhibition, drug-likeness, cytotoxicity, and selectivity properties
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