Please use this identifier to cite or link to this item: https://hdl.handle.net/11147/6296
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dc.contributor.authorKanbur, Tuğçe-
dc.contributor.authorKara, Murat-
dc.contributor.authorKutluer, Meltem-
dc.contributor.authorŞen, Ayhan-
dc.contributor.authorDelman, Murat-
dc.contributor.authorAlkan, Aylin-
dc.contributor.authorOtaş, Hasan Ozan-
dc.contributor.authorAkçok, İsmail-
dc.contributor.authorÇağır, Ali-
dc.date.accessioned2017-10-03T07:49:33Z-
dc.date.available2017-10-03T07:49:33Z-
dc.date.issued2017-
dc.identifier.citationKanbur, T., Kara, M., Kutluer, M., Şen, A., Delman, M., Alkan, A., Otaş, H. O., Akçok, İ., and Çağır, A. (2017). CRM1 inhibitory and antiproliferative activities of novel 4′-alkyl substituted klavuzon derivatives. Bioorganic and Medicinal Chemistry, 25(16), 4444-4451. doi:10.1016/j.bmc.2017.06.030en_US
dc.identifier.issn0968-0896-
dc.identifier.urihttp://doi.org/10.1016/j.bmc.2017.06.030-
dc.identifier.urihttp://hdl.handle.net/11147/6296-
dc.description.abstractKlavuzons are 6-(naphthalen-1-yl) substituted 5,6-dihydro-2H-pyran-2-one derivatives showing promising antiproliferative activities in variety of cancer cell lines. In this work, racemic syntheses of nine novel 4′-alkyl substituted klavuzon derivatives were completed in eight steps and anticancer properties of these compounds were evaluated. It is found that size of the substituent has dramatic effect over the potency and selectivity of the cytotoxic activity in cancerous and healthy pancreatic cell lines. The size of the substituent can also effect the CRM1 inhibitory properties of klavuzon derivatives. Strong cytotoxic activity and CRM1 inhibition can be observed only when a small substituent present at 4′-position of naphthalen-1-yl group. However, these substituents makes the molecule more cytotoxic in healthy pancreatic cells rather than cancerous pancreatic cells. Among the tested compounds 1,2,3,4-tetrahydrophenanthren-9-yl substituted lactone was the most cytotoxic compound and its antiproliferative activity was also tested in 3D spheroids generated from HuH-7 cell lines.en_US
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK 113Z146)en_US
dc.language.isoenen_US
dc.publisherElsevier Ltd.en_US
dc.relationinfo:eu-repo/grantAgreement/TUBITAK/KBAG/113Z146en_US
dc.relation.ispartofBioorganic and Medicinal Chemistryen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectCRM1 inhibitionen_US
dc.subjectHepatocellular carcinomaen_US
dc.subjectKlavuzonen_US
dc.subjectPancreatic canceren_US
dc.subjectAntiproliferative activityen_US
dc.subject3D cell cultureen_US
dc.titleCRM1 inhibitory and antiproliferative activities of novel 4'-alkyl substituted klavuzon derivativesen_US
dc.typeArticleen_US
dc.authoridTR106911en_US
dc.authoridTR115275en_US
dc.authoridTR110975en_US
dc.institutionauthorKanbur, Tuğçe-
dc.institutionauthorKara, Murat-
dc.institutionauthorKutluer, Meltem-
dc.institutionauthorŞen, Ayhan-
dc.institutionauthorDelman, Murat-
dc.institutionauthorAlkan, Aylin-
dc.institutionauthorOtaş, Hasan Ozan-
dc.institutionauthorAkçok, İsmail-
dc.institutionauthorÇağır, Ali-
dc.departmentIzmir Institute of Technology. Chemistryen_US
dc.identifier.volume25en_US
dc.identifier.issue16en_US
dc.identifier.startpage4444en_US
dc.identifier.endpage4451en_US
dc.identifier.wosWOS:000406023000022en_US
dc.identifier.scopus2-s2.0-85021812033en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.identifier.doi10.1016/j.bmc.2017.06.030-
dc.identifier.pmid28689976en_US
dc.relation.doi10.1016/j.bmc.2017.06.030en_US
dc.coverage.doi10.1016/j.bmc.2017.06.030en_US
item.openairetypeArticle-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.languageiso639-1en-
item.fulltextWith Fulltext-
item.grantfulltextopen-
item.cerifentitytypePublications-
crisitem.author.dept04.01. Department of Chemistry-
Appears in Collections:Chemistry / Kimya
Molecular Biology and Genetics / Moleküler Biyoloji ve Genetik
PubMed İndeksli Yayınlar Koleksiyonu / PubMed Indexed Publications Collection
Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection
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