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Acta Chim Slov ; 60(3): 628-35, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24169717

RESUMO

Protein kinase CK2 (Casein Kinase 2) is involved in cell growth; proliferation and suppression of apoptosis. Hence, it strongly promotes cell survival and can be considered an important target for human cancers. In the present study, a series of N-substituted indole-2- and 3-carboxamide derivatives were tested for inhibitions of human recombinant protein kinase CK2 to evaluate their anticancer properties. The inhibition test revealed that the most active compound 4 (1-benzyl-N-(2,4-dichlorobenzyl)-1H-indole-2-carboxamide) showed an IC50 value of 14.6 µM towards human protein kinase CK2. A molecular docking study of the compounds with CK2 was performed and revealed the binding mode of the most active compound 4, underlying its inhibitory activity.


Assuntos
Caseína Quinase II/antagonistas & inibidores , Indóis/síntese química , Inibidores de Proteínas Quinases/farmacologia , Humanos , Indóis/farmacologia , Concentração Inibidora 50 , Cinética , Modelos Moleculares , Inibidores de Proteínas Quinases/síntese química , Proteínas Recombinantes , Relação Estrutura-Atividade
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