Design, synthesis, and biological evaluation of tetrahydroquinolinones and tetrahydroquinolines with anticancer activity - Publication - Bridge of Knowledge

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Design, synthesis, and biological evaluation of tetrahydroquinolinones and tetrahydroquinolines with anticancer activity

Abstract

Colorectal cancer (CRC) is the most commonly diagnosed cancer in Europe and the United States and the second leading cause of cancer related mortality. A therapeutic strategy used for the treatment of CRC involves targeting the intracellular levels of reactive oxygen species (ROS). In this study, we synthesized a series of novel tetrahydroquinolinones and assessed their ability to inhibit CRC growth and proliferation by evoking cellular stress through ROS. Our results revealed that (2-oxo-4-phenyl- 5,6,7,8-tetrahydroquinolin-8-yl) N-(3-fluorophenyl)carbamate (20d) exhibited in vitro antiproliferative activity at micromolar concentrations. The compound also suppressed colony formation and the migration of HCT-116 cells, as well as deregulated the expression of several proteins involved in cell proliferation and metastasis. Furthermore, 20d induced massive oxidative stress by disrupting the balance of cells survival resulting in autophagy via the PI3K/AKT/mTOR signaling pathway. These findings suggest that this tetrahydroquinolinone can be an ideal lead compound for drug discovery based on quinone derivatives.

Citations

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Keywords

Details

Category:
Articles
Type:
artykuły w czasopismach
Published in:
Scientific Reports no. 12,
ISSN: 2045-2322
Language:
English
Publication year:
2022
Bibliographic description:
Ryczkowska M., Maciejewska N., Olszewski M., Witkowska M., Makowiec S.: Design, synthesis, and biological evaluation of tetrahydroquinolinones and tetrahydroquinolines with anticancer activity// Scientific Reports -Vol. 12, (2022), s.9985-
DOI:
Digital Object Identifier (open in new tab) 10.1038/s41598-022-13867-x
Sources of funding:
  • COST_FREE
Verified by:
Gdańsk University of Technology

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