Novel benzimidazole derivatives: Cytotoxic and apoptotic properties on lung cancer cell line

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dc.authorid0000-0002-0841-1299
dc.contributor.authorYurttaş, Leyla
dc.contributor.authorAkalın Çiftçi, Gülşen
dc.contributor.authorAksoy, Mehmet Onur
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned2020-11-26T06:59:48Z
dc.date.available2020-11-26T06:59:48Z
dc.date.issued2020
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.description.abstractBackground: Benzimidazole derivatives are privileged molecules known to have a wide variety of biological activities. In medicinal chemistry, due to the ring's structural similarity to nucleotides, its derivatives were investigated as new chemotherapeutic agents. Our research group have been studying 1,2-disubstituted benzimidazoles, including thiocarbamoyl group and their potential anticancer activity. Based on previous findings, we synthesized novel 1-[2-(4-substituted phenyl-2-oxoethyl)]-2-[(2/3/4-substituted phenylpiperidin-1-yl)thiocarbamoyl]benzimidazole derivatives (3a-o).Methods: The obtained fifteen derivatives were studied on A549 adenocarcinomic human alveolar basal epithelial cell line and mouse L929 fibroblastic cell line to determine their cytotoxic activity. These compounds were also investigated to identify their apoptotic properties.Results and Discussion: The structures of the compounds based on three different groups differ from each other with the phenyl substituents bonded to the piperazine ring. All of the compounds showed remarkable antitumor activity, but the first five compounds bearing non-substituted phenyl moiety exhibited selective cytotoxicity when compared in terms of potencies to the normal cell line.Conclusion: Compounds 3j, 3m and 3n were identified as the most apoptotic derivatives; however, compounds 3e and 3h provoked apoptosis with the percentages of 10.6 and 10.9% and selective cytotoxicity.
dc.identifier.citationYurttaş, L., Akalın Çiftçi, G., Akso, M. O. ve Demirayak, Ş. (2020). Novel benzimidazole derivatives: Cytotoxic and apoptotic properties on lung cancer cell line. Letters in Drug Design and Discovery, 17(10), 1227-1236. https://dx.doi.org/10.2174/157018017999200513091613
dc.identifier.doi10.2174/157018017999200513091613
dc.identifier.endpage1236
dc.identifier.issn1570-1808
dc.identifier.issn1875-628X
dc.identifier.issue10
dc.identifier.scopusqualityQ3
dc.identifier.startpage1227
dc.identifier.urihttps://dx.doi.org/10.2174/157018017999200513091613
dc.identifier.urihttps://hdl.handle.net/20.500.12511/6053
dc.identifier.volume17
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherBentham Science Publishers
dc.relation.ispartofLetters in Drug Design and Discoveryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectBenzimidazole
dc.subjectPiperazine
dc.subjectAnticancer Activity
dc.subjectA549 Lung Cancer
dc.subjectCytotoxicity
dc.subjectApoptosis
dc.titleNovel benzimidazole derivatives: Cytotoxic and apoptotic properties on lung cancer cell line
dc.typeArticle

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