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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.issued2022en_US
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-2021-0217en_US
dc.identifier.issn0939-5075
dc.identifier.issn1865-7125
dc.identifier.urihttps://doi.org/10.1515/znc-2021-0217
dc.identifier.urihttps://hdl.handle.net/20.500.12511/10022
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.en_US
dc.language.isoengen_US
dc.publisherWalter de Gruyter GmbHen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAnti-Inflammatoryen_US
dc.subjectCox-1en_US
dc.subjectCox-2en_US
dc.subjectCylooxygenaseen_US
dc.subjectPyrazoloneen_US
dc.titleNovel benzofurane-pyrazole derivatives with anti-inflammatory, cyclooxygenase inhibitory and cytotoxicity evaluationen_US
dc.typearticleen_US
dc.relation.ispartofZeitschrift fur Naturforschung - Section C Journal of Biosciencesen_US
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalıen_US
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalıen_US
dc.authorid0000-0002-5976-676Xen_US
dc.authorid0000-0003-1896-2729en_US
dc.authorid0000-0001-6047-2796en_US
dc.authorid0000-0002-0841-1299en_US
dc.identifier.volume77en_US
dc.identifier.issue7-8en_US
dc.identifier.startpage279en_US
dc.identifier.endpage285en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.identifier.doi10.1515/znc-2021-0217en_US
dc.institutionauthorŞahin, Zafer
dc.institutionauthorBiltekin, Sevde Nur
dc.institutionauthorBerk, Barkın
dc.institutionauthorDemirayak, Şeref
dc.identifier.wosqualityQ4en_US
dc.identifier.wos000744122700001en_US
dc.identifier.scopus2-s2.0-85121331949en_US
dc.identifier.pmid34902233en_US
dc.identifier.scopusqualityQ3en_US


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