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.

Department of Biotechnology and Cell Biology Medical College Faculty of Medicine University of Information Technology and Management in Rzeszow Rzeszow Poland

Department of Pharmaceutical Organic and Bioorganic Chemistry Danylo Halytsky Lviv National Medical University Lviv Ukraine

Institute of Molecular and Translational Medicine Faculty of Medicine and Dentistry Palacky University Olomouc Olomouc Czech Republic

MyeloPro Diagnostics and Research GmbH Vienna Austria

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StreaMD: the toolkit for high-throughput molecular dynamics simulations