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Chem Biodivers ; 21(3): e202301950, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38258537

RESUMO

The increased expression of VEGFR-2 in a variety of cancer cells promotes a cascade of cellular responses that improve cell survival, growth, and proliferation. Heterocycles are common structural elements in medicinal chemistry and commercially available medications that target several biological pathways and induce cell death in cancer cells. Herein, the evaluation of indazolyl-acyl hydrazones as antioxidant and anticancer agents is reported. Compounds 4e and 4j showed inhibitory activity in free radical scavenging assays (DPPH and FRPA). The titled compounds were employed in cell viability studies using MCF-7 cells, and it was observed that compounds 4f and 4j exhibited IC50 values 15.83 µM and 5.72 µM, respectively. In silico docking revealed the favorable binding energies of -7.30 kcal/mol and -8.04 kcal/mol for these compounds towards Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2), respectively. In conclusion, compounds with antioxidant activity and that target VEGFR-2 in breast cancer cells are reported.


Assuntos
Antineoplásicos , Neoplasias da Mama , Humanos , Feminino , Estrutura Molecular , Relação Estrutura-Atividade , Antioxidantes/farmacologia , Receptor 2 de Fatores de Crescimento do Endotélio Vascular , Neoplasias da Mama/tratamento farmacológico , Hidrazonas/farmacologia , Fator A de Crescimento do Endotélio Vascular/farmacologia , Proliferação de Células , Desenho de Fármacos , Simulação de Acoplamento Molecular , Antineoplásicos/química , Ensaios de Seleção de Medicamentos Antitumorais
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