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https://hdl.handle.net/11147/6296
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DC Field | Value | Language |
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dc.contributor.author | Kanbur, Tuğçe | - |
dc.contributor.author | Kara, Murat | - |
dc.contributor.author | Kutluer, Meltem | - |
dc.contributor.author | Şen, Ayhan | - |
dc.contributor.author | Delman, Murat | - |
dc.contributor.author | Alkan, Aylin | - |
dc.contributor.author | Otaş, Hasan Ozan | - |
dc.contributor.author | Akçok, İsmail | - |
dc.contributor.author | Çağır, Ali | - |
dc.date.accessioned | 2017-10-03T07:49:33Z | - |
dc.date.available | 2017-10-03T07:49:33Z | - |
dc.date.issued | 2017 | - |
dc.identifier.citation | Kanbur, 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.2017.06.030 | en_US |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | http://doi.org/10.1016/j.bmc.2017.06.030 | - |
dc.identifier.uri | http://hdl.handle.net/11147/6296 | - |
dc.description.abstract | Klavuzons 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.sponsorship | Scientific and Technological Research Council of Turkey (TUBITAK 113Z146) | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsevier Ltd. | en_US |
dc.relation | info:eu-repo/grantAgreement/TUBITAK/KBAG/113Z146 | en_US |
dc.relation.ispartof | Bioorganic and Medicinal Chemistry | en_US |
dc.rights | info:eu-repo/semantics/openAccess | en_US |
dc.subject | CRM1 inhibition | en_US |
dc.subject | Hepatocellular carcinoma | en_US |
dc.subject | Klavuzon | en_US |
dc.subject | Pancreatic cancer | en_US |
dc.subject | Antiproliferative activity | en_US |
dc.subject | 3D cell culture | en_US |
dc.title | CRM1 inhibitory and antiproliferative activities of novel 4'-alkyl substituted klavuzon derivatives | en_US |
dc.type | Article | en_US |
dc.authorid | TR106911 | en_US |
dc.authorid | TR115275 | en_US |
dc.authorid | TR110975 | en_US |
dc.institutionauthor | Kanbur, Tuğçe | - |
dc.institutionauthor | Kara, Murat | - |
dc.institutionauthor | Kutluer, Meltem | - |
dc.institutionauthor | Şen, Ayhan | - |
dc.institutionauthor | Delman, Murat | - |
dc.institutionauthor | Alkan, Aylin | - |
dc.institutionauthor | Otaş, Hasan Ozan | - |
dc.institutionauthor | Akçok, İsmail | - |
dc.institutionauthor | Çağır, Ali | - |
dc.department | İzmir Institute of Technology. Chemistry | en_US |
dc.identifier.volume | 25 | en_US |
dc.identifier.issue | 16 | en_US |
dc.identifier.startpage | 4444 | en_US |
dc.identifier.endpage | 4451 | en_US |
dc.identifier.wos | WOS:000406023000022 | en_US |
dc.identifier.scopus | 2-s2.0-85021812033 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |
dc.identifier.doi | 10.1016/j.bmc.2017.06.030 | - |
dc.identifier.pmid | 28689976 | en_US |
dc.relation.doi | 10.1016/j.bmc.2017.06.030 | en_US |
dc.coverage.doi | 10.1016/j.bmc.2017.06.030 | en_US |
dc.identifier.wosquality | Q1 | - |
dc.identifier.scopusquality | N/A | - |
item.languageiso639-1 | en | - |
item.openairetype | Article | - |
item.grantfulltext | open | - |
item.cerifentitytype | Publications | - |
item.fulltext | With Fulltext | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
crisitem.author.dept | 01. Izmir Institute of Technology | - |
crisitem.author.dept | 04.01. 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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