dc.creator | Ćurčić, Vladimir | |
dc.creator | Olszewski, Mateusz | |
dc.creator | Maciejewska, Natalia | |
dc.creator | Višnjevac, Aleksandar | |
dc.creator | Srdić-Rajić, Tatjana | |
dc.creator | Dobričić, Vladimir | |
dc.creator | García-Sosa, Alfonso T. | |
dc.creator | Kokanov, Sanja B. | |
dc.creator | Araškov, Jovana B. | |
dc.creator | Silvestri, Romano | |
dc.creator | Schüle, Roland | |
dc.creator | Jung, Manfred | |
dc.creator | Nikolić, Milan | |
dc.creator | Filipović, Nenad R. | |
dc.date.accessioned | 2023-11-28T15:34:01Z | |
dc.date.available | 2023-11-28T15:34:01Z | |
dc.date.issued | 2024 | |
dc.identifier.issn | 0365-6233 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/5298 | |
dc.description.abstract | Heterocyclic pharmacophores such as thiazole and quinoline rings have a significant role in medicinal chemistry. They are considered privileged structures since they constitute several Food and Drug Administration (FDA)-approved drugs for cancer treatment. Herein, we report the synthesis, in silico evaluation of the ADMET profiles, and in vitro investigation of the anticancer activity of a series of novel thiazolyl-hydrazones based on the 8-quinoline (1a–c), 2-quinoline (2a–c), and 8-hydroxy-2-quinolyl moiety (3a–c). The panel of several human cancer cell lines and the nontumorigenic human embryonic kidney cell line HEK-293 were used to evaluate the compound-mediated in vitro anticancer activities, leading to [2-(2-(quinolyl-8-ol-2-ylmethylene)hydrazinyl)]-4-(4-methoxyphenyl)-1,3-thiazole (3c) as the most promising compound. The study revealed that 3c blocks the cell-cycle progression of a human colon cancer cell line (HCT-116) in the S phase and induces DNA double-strand breaks. Also, our findings demonstrate that 3c accumulates in lysosomes, ultimately leading to the cell death of the hepatocellular carcinoma cell line (Hep-G2) and HCT-116 cells, by the mechanism of autophagy inhibition. | |
dc.publisher | John Wiley and Sons Inc | |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200168/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200161/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200116/RS// | |
dc.relation | AIRC IG 2020, code no. 24703. A.T.G.S. | |
dc.relation | The Estonian Research Council (PRG1509) | |
dc.relation | The Deutsche Forschungsgemeinschaft (DFG, German Research Founda- tion): SFB 992 (Project‐ID: 192904750) | |
dc.relation | CIBBS Germany's Excel- lence Strategy–EXC‐2189–Project ID: 390939984 to M.J. | |
dc.rights | restrictedAccess | |
dc.source | Archiv der Pharmazie | |
dc.subject | DNA damage | |
dc.subject | anticancer activity | |
dc.subject | hydrazonyl-thiazoles | |
dc.subject | lysosomes targeting | |
dc.subject | quinoline derivatives | |
dc.title | Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition | |
dc.type | article | |
dc.rights.license | ARR | |
dc.citation.volume | 357 | |
dc.citation.issue | 2 | |
dc.citation.spage | 2300426 | |
dc.citation.rank | M21~ | |
dc.identifier.wos | 001108118000001 | |
dc.identifier.doi | 10.1002/ardp.202300426 | |
dc.identifier.pmid | 37991233 | |
dc.identifier.scopus | 2-s2.0-85177552592 | |
dc.type.version | publishedVersion | |