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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
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.
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

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