{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,7]],"date-time":"2026-04-07T17:25:47Z","timestamp":1775582747266,"version":"3.50.1"},"reference-count":51,"publisher":"Wiley","issue":"1","license":[{"start":{"date-parts":[[2023,10,30]],"date-time":"2023-10-30T00:00:00Z","timestamp":1698624000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2024,1]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>A series of salicylidene uracil (<jats:bold>1<\/jats:bold>\u2013<jats:bold>18<\/jats:bold>) derived from 5\u2010aminouracil and substituted salicylaldehydes were analyzed for cytotoxic activity and enzyme inhibitory potency. Nine out of eighteen derivatives (<jats:bold>6\u20138<\/jats:bold>, <jats:bold>10<\/jats:bold>, <jats:bold>12\u201315<\/jats:bold>, <jats:bold>18<\/jats:bold>) are novel molecules synthesized for the first time in this work, and other derivatives were previously synthesized by our group. The compounds were characterized by Proton nuclear magnetic resonance, carbon nuclear magnetic resonance, fourier transform infrared spectroscopy, and elemental analysis. All compounds were tested for their in vitro cytotoxicity against PC\u20103 (human prostate adenocarcinoma), A549 (human alveolar adenocarcinoma), and SHSY\u20105Y (human neuroblastoma) cancer cell lines and the nontumorigenic HEK293 (human embryonic kidney cells) cell line. The 3,5\u2010di\u2010<jats:italic>tert<\/jats:italic>\u2010butylsalicylaldehyde derived compound (<jats:bold>8<\/jats:bold>) was toxic to PC\u20103 human prostate adenocarcinoma cells, showing a promising IC<jats:sub>50<\/jats:sub> value at 7.05\u2009\u00b1\u20090.76\u2009\u03bcM. The present study also aimed to evaluate the inhibitory effects of the compounds against several key enzymes, namely carbonic anhydrase I and II (CA I and CA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and glutathione reductase (GR), which are implicated in various global disorders, such as Alzheimer's disease, epilepsy, cancer, malaria, diabetes, and glaucoma. The inhibitory profiles of the tested compounds were assessed by determining their <jats:italic>K<\/jats:italic><jats:sub>i<\/jats:sub> values, which ranged from 2.96 to 9.24\u2009nM for AChE, 3.78 to 12.57\u2009nM for BChE, 8.42 to 25.74\u2009nM for CA I, 7.24 to 19.74\u2009nM for CA II, and 0.541 to 1.124\u2009\u03bcM for GR. Molecular docking studies were also performed for all compounds. Most derivatives exhibited much more effective inhibitory action compared with clinically used standards. Thus, our findings indicate that the salicylidene derivatives presented in this study are promising drug candidates that need further evaluation.<\/jats:p>","DOI":"10.1002\/ardp.202300374","type":"journal-article","created":{"date-parts":[[2023,10,30]],"date-time":"2023-10-30T13:03:29Z","timestamp":1698671009000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["Synthesis and biological evaluation of novel salicylidene uracils: Cytotoxic activity on human cancer cell lines and inhibitory action on enzymatic activity"],"prefix":"10.1002","volume":"357","author":[{"given":"Ay\u015fe Hal\u0131\u00e7","family":"Poslu","sequence":"first","affiliation":[{"name":"Department of Chemistry, Faculty of Engineering and Natural Sciences Bursa Technical University Bursa Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"\u015eafak 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