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1.
ChemMedChem ; : e202400313, 2024 Sep 11.
Article de Anglais | MEDLINE | ID: mdl-39261284

RÉSUMÉ

Flavonol-metal complexes can enhance the biological activity of flavonols. Inspired by the potential of ruthenium-based drugs in pharmaceutical applications, seven flavonol-Ru (II) complexes were synthesized to evaluate their biological activities. Among these compounds, compounds 8, 11, and 12 showed potent antioxidant activities. Compound 12 exhibited superior anti-inflammatory activity to natural quercetin, which served as a positive control. This study is the first to report the free radical scavenging abilities and antioxidant activity of flavonol-Ru (II) complexes. Furthermore, compound 12 demonstrated comparable efficacy to 5-FU against human non-small-cell lung cancer cells (A549). These results strongly support the potential of flavonol-Ru (II) agents.

2.
Arch Pharm (Weinheim) ; 357(9): e2400242, 2024 Sep.
Article de Anglais | MEDLINE | ID: mdl-38763904

RÉSUMÉ

Previously, we documented the synthesis and assessed the biological effects of chalcones containing selenium against HT-29 human colorectal adenocarcinoma cells, demonstrating their significant potential. As research on selenium-containing flavonoids remains limited, this article outlines our design and synthesis of three selenium-based flavonols and three 2-styrylchromones. We conducted evaluations of these compounds to determine their impact on human lung cancer cells (A549, H1975, CL1-0, and CL1-5) and their influence on normal lung fibroblast MRC5 cells. Additionally, we included selenium-based chalcones in our testing for comparative purposes. Our findings highlight that the simplest compound, designated as compound 1, exhibited the most promising performance among the tested molecules.


Sujet(s)
Antinéoplasiques , Chalcones , Flavonols , Humains , Antinéoplasiques/pharmacologie , Antinéoplasiques/synthèse chimique , Antinéoplasiques/composition chimique , Chalcones/pharmacologie , Chalcones/synthèse chimique , Chalcones/composition chimique , Relation structure-activité , Flavonols/pharmacologie , Flavonols/synthèse chimique , Flavonols/composition chimique , Lignée cellulaire tumorale , Prolifération cellulaire/effets des médicaments et des substances chimiques , Tests de criblage d'agents antitumoraux , Structure moléculaire , Composés organiques du sélénium/pharmacologie , Composés organiques du sélénium/synthèse chimique , Composés organiques du sélénium/composition chimique , Relation dose-effet des médicaments , 4H-1-Benzopyran-4-ones/pharmacologie , 4H-1-Benzopyran-4-ones/synthèse chimique , 4H-1-Benzopyran-4-ones/composition chimique , Survie cellulaire/effets des médicaments et des substances chimiques , Cellules A549 , Tumeurs du poumon/traitement médicamenteux , Tumeurs du poumon/anatomopathologie
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