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Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction

Abstract

The anticancer properties of quinolones is a topic of interest among researchers in the scientific world. Because these compounds do not cause side effects, unlike the commonly used cytostatics, they are considered a promising source of new anticancer drugs. In this work, we designed a brief synthetic pathway and obtained a series of novel 8-phenyltetrahydroquinolinone derivatives functionalized with benzyl-type moieties at position 3. The compounds were synthesized via classical reactions such as nucleophilic substitution, solvent lysis, and condensation. Biological evaluation revealed that 3-(1-naphthylmethyl)-4-phenyl-5,6,7,8-tetrahydro-1H-quinolin-2-one (4a) exhibited potent cytotoxicity toward colon (HTC-116) and lung (A549) cancer cell lines. Analysis of the mechanism of action of compounds showed that compound 4a induced cell cycle arrest at the G2/ M phase, leading to apoptotic cell death via intrinsic and extrinsic pathways. Taken together, the findings of the study suggest that tetrahydroquinolinone derivatives bearing a carbonyl group at position 2 could be potential lead compounds to develop anticancer agents for the treatment of lung cancers

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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.: Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction// Scientific Reports -Vol. 12,iss. 1 (2022), s.19076-
DOI:
Digital Object Identifier (open in new tab) 10.1038/s41598-022-23640-9
Sources of funding:
  • Free publication
Verified by:
Gdańsk University of Technology

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