dc.contributor.author | Tapera,Michael | |
dc.contributor.author | Kekeçmuhammed, Hüseyin | |
dc.contributor.author | Tüzün,Burak | |
dc.contributor.author | Sarıpınar,Emin | |
dc.contributor.author | Koçyiğit,Ümit M. | |
dc.contributor.author | Yıldırım,Ebrar | |
dc.contributor.author | Doğan, Murat | |
dc.contributor.author | Zorlu, Yunus | |
dc.date.accessioned | 2023-06-21T12:08:01Z | |
dc.date.available | 2023-06-21T12:08:01Z | |
dc.date.issued | 2022/12/05 | tr |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0022286022014703 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/13842 | |
dc.description.abstract | A new series of imidazolyl hydrazone derivatives IA (1-12) were prepared from a condensation reaction between indoline-2,3-dione (isatin) and 2-benzylidenehydrazinecarboximidamide derivatives. The structure of compounds was elucidated using various spectral techniques including FTIR, 1H NMR, 13C NMR, and HRMS. The proposed structure of IA-2 was determined by single-crystal X-ray analysis. Synthesized compounds were evaluated for their inhibitory action against carbonic anhydrase I and II isoenzymes (hCA I and hCA II), as well as cytotoxicity activity in a cancer cell line (HT-29) and a healthy cell line (NIH 3T3). Among them, some compounds exhibited remarkable CA inhibitory activities compared to a standard inhibitor with Ki values in the range of 13.434 ± 3.278-522.549 ± 360.720 nM for hCA I (Ki value for standard inhibitor = 271.15 ± 74.620 nM) and 41.108 ± 10.180-271.171 ± 65.293 nM for hCA II (Ki value for standard inhibitor = 113.07 ± 20.980 nM) and significant antiproliferative activity with less toxicity to a health cell line. In addition, the theoretical parameters of the bioactive molecules were calculated to establish their drug-likeness qualities and ADME/T analysis was carried out to examine the drug properties of the synthesized compounds. | tr |
dc.language.iso | eng | tr |
dc.publisher | Elsevier | tr |
dc.rights | info:eu-repo/semantics/openAccess | tr |
dc.title | Synthesis, carbonic anhydrase inhibitory activity, anticancer activity and molecular docking studies of new imidazolyl hydrazone derivatives | tr |
dc.type | article | tr |
dc.relation.journal | Journal of Molecular Structure | tr |
dc.contributor.department | Eczacılık Fakültesi | tr |
dc.contributor.authorID | 0000-0001-8710-2912 | tr |
dc.identifier.issue | 1269 | tr |
dc.identifier.endpage | 133816 | tr |
dc.identifier.startpage | 133816 | tr |
dc.relation.publicationcategory | Ulusal Hakemli Dergide Makale - Kurum Öğretim Elemanı | tr |