Novel benzofurane-pyrazole derivatives with anti-inflammatory, cyclooxygenase inhibitory and cytotoxicity evaluation

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dc.authorid0000-0002-5976-676X
dc.authorid0000-0003-1896-2729
dc.authorid0000-0001-6047-2796
dc.authorid0000-0002-0841-1299
dc.contributor.authorŞahin, Zafer
dc.contributor.authorÖzhan, Yağmur
dc.contributor.authorSipahi, Hande
dc.contributor.authorBiltekin, Sevde Nur
dc.contributor.authorYurttaş, Leyla
dc.contributor.authorBerk, Barkın
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned2022-11-23T12:53:09Z
dc.date.available2022-11-23T12:53:09Z
dc.date.issued2022
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalı
dc.description.abstractNovel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory and cytotoxic properties. 4-(2-chloroacetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one were reacted with alpha-hydroxy aldehyde or alpha-hydroxy ketone derivatives to obtain nine novel pyrazolone derivatives. Structures were successfully elucidated by H-1 NMR, C-13 NMR, IR and HRMS. Enzyme inhibitory activity was measured on cyclooxygenases (COXs) as considered to address anti-inflammatory activity. Compound 2 showed the highest activity on both COX-1 and COX-2 subtypes with 12.0 mu M and 8.0 mu M IC50, respectively. This activity was found close to indomethacin COX-2 inhibition measured as 7.4 mu M IC50. Rest of the compounds (1, 3-9) showed 10.4-28.1 mu M IC50 on COX-2 and 17.0-35.6 mu M IC50 on COX-1 (Compound 1 has no activity on COX-1). Tested compounds (1-9) showed activity on NO production. Only compound was the 4, which showed a low inhibition on IL-6 levels. Cell viability was up to 60% at 100 mu M for all compounds (1-9) on RAW 264.7 and NIH3T3 cell lines, thus compounds were reported to be noncytotoxic.
dc.identifier.citationŞahin, Z., Özhan, Y., Sipahi, H., Biltekin, S. N., Yurttaş, L., Berk, B. ... Demirayak, Ş. (2022). Novel benzofurane-pyrazole derivatives with anti-inflammatory, cyclooxygenase inhibitory and cytotoxicity evaluation. Zeitschrift fur Naturforschung - Section C Journal of Biosciences, 77(7-8), 279-285. https://doi.org/10.1515/znc-2021-0217
dc.identifier.doi10.1515/znc-2021-0217
dc.identifier.endpage285
dc.identifier.issn0939-5075
dc.identifier.issn1865-7125
dc.identifier.issue45511
dc.identifier.pmid34902233
dc.identifier.scopus2-s2.0-85121331949
dc.identifier.scopusqualityQ3
dc.identifier.startpage279
dc.identifier.urihttps://doi.org/10.1515/znc-2021-0217
dc.identifier.urihttps://hdl.handle.net/20.500.12511/10022
dc.identifier.volume77
dc.identifier.wos000744122700001en_US
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.institutionauthorŞahin, Zafer
dc.institutionauthorBiltekin, Sevde Nur
dc.institutionauthorBerk, Barkın
dc.institutionauthorDemirayak, Şeref
dc.language.isoen
dc.publisherWalter de Gruyter GmbH
dc.relation.ispartofZeitschrift fur Naturforschung - Section C Journal of Biosciencesen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectAnti-Inflammatory
dc.subjectCox-1
dc.subjectCox-2
dc.subjectCylooxygenase
dc.subjectPyrazolone
dc.titleNovel benzofurane-pyrazole derivatives with anti-inflammatory, cyclooxygenase inhibitory and cytotoxicity evaluation
dc.typeArticle

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