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Chem Biodivers ; 20(2): e202200807, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-36302719

RESUMEN

In this study, eight naphthoquinone derivatives were synthesized in yields ranging from 52 to 96% using easy, fast, and low-cost methodologies. All naphthoquinone derivatives were screened for their in vitro anti-proliferative activities against OVCA A2780 cancer cell lines. Amongst all analysed compounds, derivatives 3-5 presented the most prominent cytotoxic potential. Naphthoquinones 3 and 4, bearing sulfur-containing groups, were identified as having high potential for ROS production, in particular the superoxide anion. Furthermore, 3 and 4 compounds caused a decrease in the cell population in G0/G1 and induced more than 90% of the cell population to apoptosis. Compound 5 did not act in any of these processes. Finally, compounds 3-5 were tested for their inhibitory ability against PI3K and MAPK. Compounds 3 and 4 do not inhibit the PI3K enzyme. On the other hand, the naphthoquinone-polyphenol 5 was only able to inhibit the percentage of cells expressing pERK.


Asunto(s)
Antineoplásicos , Naftoquinonas , Neoplasias Ováricas , Humanos , Femenino , Línea Celular Tumoral , Naftoquinonas/farmacología , Antineoplásicos/farmacología , Fosfatidilinositol 3-Quinasas/metabolismo , Proliferación Celular , Relación Estructura-Actividad
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