Synthesis and cytotoxicity studies on new pyrazolecontaining oxime ester derivatives

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dc.authorscopusid6602307926
dc.authorscopusid57203395057
dc.authorscopusid56779753300
dc.authorscopusid56779707700
dc.authorscopusid57213636835
dc.authorscopusid26436187600
dc.contributor.authorKarakurt A.
dc.contributor.authorBozbey I.
dc.contributor.authorUslu H.
dc.contributor.authorSari S.
dc.contributor.authorOzdemir Z.
dc.contributor.authorSalva E.
dc.date.accessioned2024-08-04T20:02:32Z
dc.date.available2024-08-04T20:02:32Z
dc.date.issued2021
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 ?M. Of these, compound 7a was the most active combination with an IC50 value of 85.94 ?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 druglike while their pharmacokinetic features were also encouraging, and were in line with in silico predictions. © 2019 The authors.en_US
dc.description.sponsorshipInönü Üniversitesi: 2011/65en_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.scopus2-s2.0-85108378815en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage1315en_US
dc.identifier.urihttps://doi.org/10.4314/TJPR.V18I6.24
dc.identifier.urihttps://hdl.handle.net/11616/91749
dc.identifier.volume18en_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherUniversity of Beninen_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 pyrazolecontaining oxime ester derivativesen_US
dc.typeArticleen_US

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