Synthesis and cytotoxicity studies on new pyrazole-containing oxime ester derivatives

Basit Öğe Kaydı
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridUSLU, HARUN/0000-0001-8827-8557
dc.authoridBozbey Merde, İrem/0000-0002-9290-938X
dc.authoridKarakurt, Arzu/0000-0003-2209-0871
dc.authoridSalva, Emine/0000-0002-1159-5850
dc.authoridOzdemir, Zenyep/0000-0003-4559-2305
dc.authoridŞALVA, EMINE/0000-0002-1159-5850
dc.authorwosidSARI, SUAT/A-5249-2017
dc.authorwosidUSLU, HARUN/P-3681-2019
dc.authorwosidBozbey Merde, İrem/HCI-8239-2022
dc.authorwosidKarakurt, Arzu/ABH-9340-2020
dc.authorwosidSalva, Emine/ABI-2766-2020
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.authorwosidŞALVA, EMINE/CAH-3062-2022
dc.contributor.authorKarakurt, Arzu
dc.contributor.authorBozbey, Irem
dc.contributor.authorUslu, Harun
dc.contributor.authorSari, Suat
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorSalva, Emine
dc.date.accessioned2024-08-04T21:01:16Z
dc.date.available2024-08-04T21:01:16Z
dc.date.issued2019
dc.departmentİnönü Üniversitesien_US
dc.description.abstractPurpose: To synthesize a series of new 1-(2-naphthyl)-2-(1H-pyrazol-1-yl)ethanone oxime ester derivatives (5-12) with potential anticancer properties, and to determine their cytotoxic effects in mouse fibroblast and human neuroblastoma cell lines. Methods: The title compounds were obtained through sodium salt reaction of 1-(naphthalene-2-yl)-2(1H-pyrazol-1-yl)etanone oxime (4) with various acyl chlorides. The cytotoxic effects were evaluated by MTS colorimetric assay, while physicochemical descriptors were calculated using QikProp software. Results: Most of the compounds showed approximately 50 - 60 % inhibition against SH-SY5Y neuroblastoma cells at 100 mu M. Of these, compound 7a was the most active combination with an IC50 value of 85.94 mu M. The toxic effect of the compounds on mouse fibroblast cell line was insignificant (p < 0.05) even when the dose was increased. The calculated physicochemical properties of the compounds were within drug-like chemical space. Conclusion: The synthesized oxime ester derivatives with pyrazole ring exhibit selective toxicity to neuroblastoma cells without affecting healthy mouse fibroblast cells. The compounds proved to be drug-like while their pharmacokinetic features were also encouraging, and were in line with in silico predictions.en_US
dc.description.sponsorshipInonu University Scientific Research Projects Coordination Unit [2011/65]en_US
dc.description.sponsorshipThis work was supported by Inonu University Scientific Research Projects Coordination Unit (Project no. 2011/65).en_US
dc.identifier.doi10.4314/tjpr.v18i6.24
dc.identifier.endpage1322en_US
dc.identifier.issn1596-5996
dc.identifier.issue6en_US
dc.identifier.startpage1315en_US
dc.identifier.urihttps://doi.org/10.4314/tjpr.v18i6.24
dc.identifier.urihttps://hdl.handle.net/11616/104244
dc.identifier.volume18en_US
dc.identifier.wosWOS:000473329600024en_US
dc.identifier.wosqualityQ4en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.language.isoenen_US
dc.publisherPharmacotherapy Groupen_US
dc.relation.ispartofTropical Journal of Pharmaceutical Researchen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectCytotoxic activityen_US
dc.subjectE/Z isomeren_US
dc.subjectNeuroblastoma cellen_US
dc.subjectOxime esteren_US
dc.subjectPyrazoleen_US
dc.titleSynthesis and cytotoxicity studies on new pyrazole-containing oxime ester derivativesen_US
dc.typeArticleen_US

Dosyalar

Koleksiyon

WoS İndeksli Yayınlar Koleksiyonu