The stilbene and dibenzo[b,f]oxepine derivatives as anticancer compounds
Authors:
- Damian Garbicz,
- Piotr Tobiasz,
- Filip Borys,
- Tomasz Pilżys,
- Michał Marcinkowski,
- Marcin Poterała,
- Elżbieta Grzesiuk,
- Hanna Krawczyk
Abstract
In the present study, the synthesis and cytotoxic effect of six stilbenes and three oxepine derivatives against two cancerous – HeLa and U87, and two normal – EUFA30 and HEK293 cell lines has been reported. The results of cytotoxic assay and flow 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 and their 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 more weakly with tubulin, relative to colchicine but they act more selectively towards cancerous versus normal cell lines. Obtained results proved that the compounds that are the most active against cancerous cells operate through tubulin binding.
- Record ID
- WUTaf621a59e47b4aca9ea922504128680d
- Author
- Journal series
- Biomedicine & Pharmacotherapy, ISSN 0753-3322, e-ISSN 1950-6007
- Issue year
- 2020
- Vol
- 123
- Pages
- 1-9
- Publication size in sheets
- 0.30
- Article number
- 109781
- ASJC Classification
- ;
- DOI
- DOI:10.1016/j.biopha.2019.109781 Opening in a new tab
- URL
- https://www.sciencedirect.com/science/article/pii/S0753332219354034 Opening in a new tab
- Language
- (en) English
- License
- File
-
- File: 1
- The stilbene and dibenzo[b,f]oxepine derivatives as anticancer compounds, File wdpb_publikacje_pliki_plik_publikacja_4135_org.pdf / 1 MB
- wdpb_publikacje_pliki_plik_publikacja_4135_org.pdf
- publication date: 17-01-2021
- The stilbene and dibenzo[b,f]oxepine derivatives as anticancer compounds, File wdpb_publikacje_pliki_plik_publikacja_4135_org.pdf / 1 MB
-
- Score (nominal)
- 100
- Score source
- journalList
- Score
- = 100.0, 11-05-2022, ArticleFromJournal
- Publication indicators
- = 4; = 2; : 2018 = 0.951; : 2020 (2 years) = 6.530 - 2020 (5 years) =5.980
Share
- Uniform Resource Identifier
- https://repo.pw.edu.pl/info/article/WUTaf621a59e47b4aca9ea922504128680d/
- URN
urn:pw-repo:WUTaf621a59e47b4aca9ea922504128680d
* presented citation count is obtained through Internet information analysis and it is close to the number calculated by the Publish or PerishOpening in a new tab system.