Synthesis and Antiproliferative Effect of Halogenated Coumarin Derivatives

A series of 6- and 6,8-halocoumarin derivatives have been investigated as potential antiproliferative compounds against a panel of tumor and normal cell lines. Cytotoxic effects were determined by the MTT method. To investigate the potential molecular mechanism involved in the cytotoxic effect, apop...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2022-12, Vol.27 (24), p.8897
Main Authors: Dettori, Tinuccia, Sanna, Giuseppina, Cocco, Andrea, Serreli, Gabriele, Deiana, Monica, Palmas, Vanessa, Onnis, Valentina, Pilia, Luca, Melis, Nicola, Moi, Davide, Caria, Paola, Secci, Francesco
Format: Article
Language:English
Subjects:
Analysis
Antineoplastic Agents - pharmacology
Antioxidants
antiproliferative activity
Antiproliferatives
Apoptosis
Cell cycle
Cell growth
Cell Line, Tumor
Cell Proliferation
Coumarin
Coumarins
Coumarins - pharmacology
Cytotoxicity
Development and progression
Drug Screening Assays, Antitumor
Humans
Instrument industry
Investigations
Kinases
Oxidation
Reactive oxygen species
Reactive Oxygen Species - metabolism
ROS
S phase
Thyroid cancer
Thyroid Neoplasms - pathology
TPC-1 cells
Tumor cell lines
Tumors
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Summary:A series of 6- and 6,8-halocoumarin derivatives have been investigated as potential antiproliferative compounds against a panel of tumor and normal cell lines. Cytotoxic effects were determined by the MTT method. To investigate the potential molecular mechanism involved in the cytotoxic effect, apoptosis assay, cell cycle analysis, reactive oxygen species (ROS), and reduced glutathione analysis were performed. Among the screened compounds, coumarins 6,8-dibromo-2-oxo-2 -chromene-3-carbonitrile and 6,8-diiodo-2-oxo-2 -chromene-3-carbonitrile exhibited the most antiproliferative effect in thyroid cancer-derived cells TPC-1. The apoptosis assay showed that both and induced apoptosis in TPC-1 thyroid cancer cells. According to these experiments, both coumarins induced a slight increase in TPC-1 cells in the G2/M phase and a decrease in the S phase. A significant increase in ROS levels was observed in TPC-1 treated with diiodocoumarin , while the dibromocoumarin induced a decrease in ROS in a dose and time-dependent manner.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules27248897