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Pharmazie ; 73(4): 191-195, 2018 04 02.
Artigo em Inglês | MEDLINE | ID: mdl-29609684

RESUMO

Protein kinase CK2 is a potential drug target for many diseases including cancer, inflammatory disorders, Alzheimer's disease, Parkinson's disease and viral infections. Significant efforts have been made for the discovery of potent inhibitors of this enzyme. Herein, we report on the synthesis, characterization, and biological evaluation of novel flavonoid compounds as CK2 inhibitors. The tested compounds were 2 (4`-hydroxynaphthyl) chromen-4-one which is a naphthyl backbone flavonoid with an IC50 value of 0.45±0.059 µM and 2(4-hydroxyphenyl)-4H-chromen-4-one a phenyl based derivative with an IC50 value of 0.33±0.048 µM. Cell viability was tested using MCF-7 cells. Both compounds were able to reduce the cell viability around 50 % in concentration of 100 µM after 48 h. Molecular modeling studies were performed to understand the binding mode of both compounds.


Assuntos
Benzopiranos/síntese química , Benzopiranos/farmacologia , Caseína Quinase II/antagonistas & inibidores , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/farmacologia , Caseína Quinase II/química , Proliferação de Células/efeitos dos fármacos , Desenho de Fármacos , Humanos , Células MCF-7 , Modelos Moleculares , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade
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