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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.
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Authors (14)
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Vladimir Ćurčić
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Aleksandar Višnjevac
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Tatjana Srdić-rajić
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Vladimir Dobričić
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Alfonso T García-sosa
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Sanja B Kokanov
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Jovana B. Araškov
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Romano Silvestri
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Roland Schüle
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Manfred Jung
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Milan Nikolić
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Nenad R. Filipovići
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Details
- Category:
- Articles
- Type:
- artykuły w czasopismach
- Published in:
-
ARCHIV DER PHARMAZIE
no. 357,
pages 1 - 18,
ISSN: 0365-6233 - Language:
- English
- Publication year:
- 2024
- Bibliographic description:
- Ćurčić V., Olszewski M., Maciejewska N., Višnjevac A., Srdić-Rajić T., Dobričić V., García-Sosa A. T., Kokanov S. B., Araškov J. B., Silvestri R., Schüle R., Jung M., Nikolić M., Filipovići N. R.: Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition// ARCHIV DER PHARMAZIE -Vol. 357,iss. 2 (2024), s.1-18
- DOI:
- Digital Object Identifier (open in new tab) 10.1002/ardp.202300426
- Sources of funding:
-
- Free publication
- Verified by:
- Gdańsk University of Technology
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