Anticancer 5-arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones as tubulin inhibitors

. 2022 Dec ; 355 (12) : e2200419. [epub] 20220915

Jazyk angličtina Země Německo Médium print-electronic

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/pmid36109178

Grantová podpora
CZ.02.1.01/0.0/0.0/16_019/0000868 European Regional Development Fund
CZ-OPENSCREEN Czech Ministry of Education, Youth and Sports
LM2018130 Czech Ministry of Education, Youth and Sports
EATRIS-CZ Czech Ministry of Education, Youth and Sports
LM2018133 Czech Ministry of Education, Youth and Sports
2020.02/0035 National Research Foundation of Ukraine
0121U100690 Ministry of Healthcare of Ukraine

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.

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