Synthesis and antiproliferative evaluation of novel 3,5,8-trisubstituted coumarins against breast cancer.
Future Med Chem
; 16(11): 1053-1073, 2024.
Article
em En
| MEDLINE
| ID: mdl-38708686
ABSTRACT
Aim:
This study focused on designing and synthesizing novel derivatives of 3,5,8-trisubstituted coumarin.Results:
The synthesized compounds, particularly compound 5, exhibited significant cytotoxic effects on MCF-7 cells, surpassing staurosporine, and reduced toxicity toward MCF-10A cells, highlighting potential pharmacological advantages. Further, compound 5 altered the cell cycle and significantly increased apoptosis in MCF-7 cells, involving both early (41.7-fold) and late stages (33-fold), while moderately affecting necrotic signaling. The antitumor activity was linked to a notable reduction (4.78-fold) in topoisomerase IIß expression. Molecular modeling indicated compound 5's strong affinity for EGFR, human EGF2 and topoisomerase II proteins.Conclusion:
These findings highlight compound 5 as a multifaceted antitumor agent for breast cancer.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Neoplasias da Mama
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Ensaios de Seleção de Medicamentos Antitumorais
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Apoptose
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Cumarínicos
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Proliferação de Células
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Antineoplásicos
Limite:
Female
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Humans
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article