Synthesis of new piperazine‐oxadiazole derivatives and investigation of their anticancer activities

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dc.authorid0009-0000-8412-0242
dc.authorid0000-0001-8827-8557
dc.authorid0000-0003-2345-7313
dc.authorid0000-0001-5948-1855
dc.authorid0000-0002-0151-6266
dc.contributor.authorUslu, Harun
dc.contributor.authorGöktaş, Bünyamin
dc.contributor.authorOsmaniye, Derya
dc.contributor.authorLevent, Serkan
dc.contributor.authorPeçe Göktaş, Sare
dc.contributor.authorSağlık Özkan, Begüm Nurpelin
dc.contributor.authorÖzkay, Yusuf
dc.contributor.authorBenkli, Kadriye
dc.date.accessioned2024-10-18T07:29:23Z
dc.date.available2024-10-18T07:29:23Z
dc.date.issued2025
dc.departmentFakülteler, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.description.abstractSince cancer is one of the leading causes of human death, recent research has largely focused on developing multi-target drug designs. In this study, we designed and synthesized a series of piperazine-oxadiazole derivatives as aromatase inhibitors for the treatment of cancer. Their structures were confirmed by 1 C NMR, HRMS and FTIR spectroscopic methods. Cytotoxicity (MTT) was performed to determine the anticancer activity of the compounds as aromatase inhibitors against breast (MCF7), fibroblast (NIH3T3) and lung (A549) cell lines. Letrazol was used as the reference agent, compound 4b exhibited a significant effect among other derivatives with a value of IC H NMR, 50 =2.103±0.088 μ 13 Magainst the MCF7 cell line. Docking study showed that 4b was one of the compounds with the best pose on the aromatase. The docking study showed that 4e was one of the compounds that gave the best pose on EGFR and topoisomerase. When the aromatase, EGFR and topoisomerase docking results were compared, it was concluded that our synthesized compounds may be more effective on the Aromatase macromolecule. From the obtained evaluations of the designed batches, compound 4b appeared to be a promising agent as an aromatase inhibitor for further research and evaluation studies in the future.
dc.description.sponsorshipAnadolu University Faculty of Pharmacy Central Research Laboratory (MERLAB)
dc.identifier.citationUslu, H., Göktaş, B., Osmaniye, D., Levent, S., Peçe Göktaş, S., Sağlık Özkan, B. N., Özkay, Y., & Benkli, K. (2025). Synthesis of new piperazine‐oxadiazole derivatives and investigation of their anticancer activities. Journal of Molecular Structure, 1322, pp. 1-12. https://doi.org/10.1016/j.molstruc.2024.140298
dc.identifier.doi10.1016/j.molstruc.2024.140298
dc.identifier.endpage11
dc.identifier.issn1872-8014
dc.identifier.issn0022-2860
dc.identifier.scopus2-s2.0-85206075877
dc.identifier.scopusqualityQ1
dc.identifier.startpage1
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2024.140298
dc.identifier.urihttps://hdl.handle.net/20.500.13055/828
dc.identifier.volume1322
dc.identifier.wosWOS:001335201200001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.indekslendigikaynak.otherSCI-E - Science Citation Index Expanded
dc.institutionauthorBenkli, Kadriye
dc.institutionauthorid0009-0000-8412-0242
dc.language.isoen
dc.publisherElsevier
dc.relation.ispartofJournal of Molecular Structure
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectAnticancer
dc.subjectCytotoxcicity
dc.subjectOxadiazole
dc.subjectPiperazine
dc.subjectAromatase
dc.subjectTopoisomerase
dc.subjectEGFR
dc.titleSynthesis of new piperazine‐oxadiazole derivatives and investigation of their anticancer activities
dc.typeArticle
dspace.entity.typePublication

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