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The stilbene and dibenzo[b,f]oxepine derivatives as anticancer compounds

Garbicz, Damian and Tobiasz, Piotr and Borys, Filip and Pilżys, Tomasz and Marcinkowski, Michał and Poterała, Marcin and Grzesiuk, Elzbieta and Krawczyk, Hanna (2020) The stilbene and dibenzo[b,f]oxepine derivatives as anticancer compounds. Biomedicine & Pharmacotherapy, 123 . p. 109781. ISSN 0753-3322

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Official URL: https://www.sciencedirect.com/science/article/pii/...


In the present study, the synthesis and cytotoxic effect of six stilbenes and three oxepine derivatives against twocancerous–HeLa and U87, and two normal–EUFA30 and HEK293 cell lines has been reported. The results ofcytotoxic assay andflow cytometry analysis revealed that compounds 9-nitrobenzo[b]naphtho[1,2-f]oxepine(4), (E)-3,3′,4,4′,5,5′-hexamethoxystilbene (6) and 4-hydroxy-2′,4′-dinitrostilbene (8) were the most active andtheir interaction with tubulin (crystal structure from PDB) has been analyzed by computer molecular modeling.Molecular docking of these compounds on colchicine binding site of the tubulin indicates the interaction of (4),(6) and (8) with tubulin. The compound (4) could interact stronger with tubulin, relative to colchicine, however,with no selectivity of action against cancer and normal cells. Conversely, compounds (6) and (8) interact moreweakly with tubulin, relative to colchicine but they act more selectively towards cancerous versus normal celllines. Obtained results proved that the compounds that are the most active against cancerous cells operatethrough tubulin binding.

Item Type:Article
Subjects:Q Science > QD Chemistry
Q Science > QH Natural history > QH301 Biology
Divisions:Department of Molecular Biology
ID Code:1801
Deposited By: Prof. Elżbieta Grzesiuk
Deposited On:20 Dec 2019 10:53
Last Modified:20 Dec 2019 10:53

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