Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity

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dc.authoridOzakpınar, Ozlem Bingol/0000-0003-0287-5639
dc.authoridKüçükgüzel, İlkay/0000-0002-7188-1859
dc.authoridHelvacioglu Akyuz, Sinem/0000-0002-3144-5024
dc.authoridCIFTCI, GAMZE/0000-0001-7138-8012
dc.authoridGURBOGA, MERVE/0000-0003-4614-7094
dc.authoridYelekci, Kemal/0000-0002-0052-4926
dc.authoridSahin, Fikrettin/0000-0003-1503-5567
dc.authorwosidOzakpınar, Ozlem Bingol/ABI-4144-2020
dc.authorwosidbülbül, bahadır/HDM-7433-2022
dc.authorwosidKüçükgüzel, İlkay/Z-1541-2019
dc.authorwosidÖzakpınar, Özlem Bingöl/ACB-1160-2022
dc.authorwosidHelvacioglu Akyuz, Sinem/GWQ-9714-2022
dc.authorwosidYelekci, Kemal/B-1431-2019
dc.contributor.authorBülbül, Bahadır
dc.contributor.authorDing, Kai
dc.contributor.authorZhan, Chang-Guo
dc.contributor.authorÇftçi, Gamze
dc.contributor.authorYelekci, Kemal
dc.contributor.authorGürboğa, Merve
dc.contributor.authorÖzakpınar, Özlem Bingöl
dc.date.accessioned2023-07-26T11:50:53Z
dc.date.available2023-07-26T11:50:53Z
dc.date.issued2022
dc.departmentDÜ, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümüen_US
dc.description.abstractSome novel triazole-bearing ketone and oxime derivatives were synthesized from Ibuprofen. In vitro cytotoxic activities of all synthesized molecules against five cancer lines (human breast cancer MCF-7, human lung cancer A549, human prostate cancer PC-3, human cervix cancer HeLa, and human chronic myelogenous leukemia K562 cell lines) were evaluated by MTT assay. In addition, mouse embryonic fibroblast cells (NIH/3T3) were also evaluated to determine the selectivity. Compounds 18, 36, and 45 were found to be the most cytotoxic, and their IC50 values were in the range of 17.46-68.76 mu M, against the tested cancer cells. According to the results, compounds 7 and 13 demonstrated good anti-inflammatory activity against the microsomal enzyme prostaglandin E2 synthase-1 (mPGES-1) enzyme at IC50 values of 13.6 and 4.95 mu M. The low cytotoxicity and non-mutagenity of these compounds were found interesting. Also, these compounds significantly prevented tube formation in angiogenesis studies. In conclusion, the anti-inflammatory and angiogenesis inhibitory activities of these compounds without toxicity suggested that they may be promising agents in anti-inflammatory treatment and they may be supportive agents for the cancer treatment. [GRAPHICS] .en_US
dc.description.sponsorshipMarmara University Scientific Research Projects Coordination Unit [SAG-A-070617-0336]en_US
dc.description.sponsorshipThis work has been supported by Marmara University Scientific Research Projects Coordination Unit under grant number SAG-A-070617-0336.en_US
dc.identifier.doi10.1007/s11030-022-10551-0
dc.identifier.issn1381-1991
dc.identifier.issn1573-501X
dc.identifier.pmid36331786en_US
dc.identifier.scopus2-s2.0-85141412569en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1007/s11030-022-10551-0
dc.identifier.urihttps://hdl.handle.net/20.500.12684/12449
dc.identifier.wosWOS:000878961700002en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakPubMeden_US
dc.indekslendigikaynakScopusen_US
dc.institutionauthorBülbül, Bahadır
dc.language.isoenen_US
dc.publisherSpringeren_US
dc.relation.ispartofMolecular Diversityen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmz$2023V1Guncelleme$en_US
dc.subject1,2,4-Triazole; Atropisomer; Diastereotope; X-Ray Diffraction; Cancer; Angiogenesis; Mpges-1; Cytotoxicityen_US
dc.subjectProstaglandin-E Synthase-1; Antiinflammatory Activity; Hybrids Synthesis; Beta-Catenin; Tumor-Growth; Derivatives; Cox-2; Discovery; Design; Antibacterialen_US
dc.titleNovel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activityen_US
dc.typeArticleen_US

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