Search
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.
Citations
-
2
CrossRef
-
0
Web of Science
-
2
Scopus
Authors (14)
-
Vladimir Ćurčić
-
Aleksandar Višnjevac
-
Tatjana Srdić-rajić
-
Vladimir Dobričić
-
Alfonso T García-sosa
-
Sanja B Kokanov
-
Jovana B. Araškov
-
Romano Silvestri
-
Roland Schüle
-
Manfred Jung
-
Milan Nikolić
-
Nenad R. Filipovići
Cite as
Full text
full text is not available in portal
Keywords
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
seen 58 times
Recommended for you
Synthesis, Molecular Structure, Anticancer Activity, and QSAR Study of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)Benzenesulfonamide Derivatives
- B. Żołnowska,
- J. Sławiński,
- Z. Brzozowski
- + 5 authors
Novel N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives: synthesis and anticancer activity evaluation
- A. Bułakowska,
- J. Sławiński,
- K. Siedlecka-Kroplewska
- + 3 authors