Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition - Publikacja - MOST Wiedzy

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Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition

Abstrakt

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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Kategoria:
Publikacja w czasopiśmie
Typ:
artykuły w czasopismach
Opublikowano w:
ARCHIV DER PHARMAZIE nr 357, strony 1 - 18,
ISSN: 0365-6233
Język:
angielski
Rok wydania:
2024
Opis bibliograficzny:
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:
Cyfrowy identyfikator dokumentu elektronicznego (otwiera się w nowej karcie) 10.1002/ardp.202300426
Źródła finansowania:
  • COST_FREE
Weryfikacja:
Politechnika Gdańska

wyświetlono 24 razy

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