Please use this identifier to cite or link to this item:
https://hdl.handle.net/11147/6296
Title: | CRM1 inhibitory and antiproliferative activities of novel 4'-alkyl substituted klavuzon derivatives | Authors: | Kanbur, Tuğçe Kara, Murat Kutluer, Meltem Şen, Ayhan Delman, Murat Alkan, Aylin Otaş, Hasan Ozan Akçok, İsmail Çağır, Ali |
Keywords: | CRM1 inhibition Hepatocellular carcinoma Klavuzon Pancreatic cancer Antiproliferative activity 3D cell culture |
Publisher: | Elsevier Ltd. | Source: | 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 | 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. | URI: | http://doi.org/10.1016/j.bmc.2017.06.030 http://hdl.handle.net/11147/6296 |
ISSN: | 0968-0896 |
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 |
Show full item record
CORE Recommender
SCOPUSTM
Citations
7
checked on Sep 1, 2024
WEB OF SCIENCETM
Citations
7
checked on Aug 24, 2024
Page view(s)
536
checked on Sep 2, 2024
Download(s)
338
checked on Sep 2, 2024
Google ScholarTM
Check
Altmetric
Items in GCRIS Repository are protected by copyright, with all rights reserved, unless otherwise indicated.