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Anticancer 5-arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones as tubulin inhibitors
J. Rehulka, I. Subtelna, A. Kryshchyshyn-Dylevych, A. Cherniienko, A. Ivanova, M. Matveieva, P. Polishchuk, S. Gurska, M. Hajduch, O. Zagrijtschuk, P. Dzubak, R. Lesyk
Jazyk angličtina Země Německo
Typ dokumentu časopisecké články
PubMed
36109178
DOI
10.1002/ardp.202200419
Knihovny.cz E-zdroje
- MeSH
- apoptóza MeSH
- modulátory tubulinu * farmakologie chemie MeSH
- nádorové buněčné linie MeSH
- proliferace buněk MeSH
- protinádorové látky * farmakologie chemie MeSH
- screeningové testy protinádorových léčiv MeSH
- tubulin metabolismus MeSH
- vazebná místa MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Publikační typ
- časopisecké články MeSH
Studying the anticancer activity of 5-arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones towards cell lines of different cancer types allowed the identification of hit-compounds inhibiting the growth of daunorubicin- (CEM-DNR, IC50 = 0.32-1.28 μM) and paclitaxel-resistant (K562-TAX, IC50 = 0.21-1.23 μM) cell lines, with favorable therapeutic indexes. The studied compounds induced apoptosis and cellular proliferation in treated CCRF-CEM cells. The hit compounds were shown to induce mitotic arrest by interacting with tubulin, inhibiting its polymerization by binding to the colchicine binding site.
Citace poskytuje Crossref.org
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