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Bioorg Med Chem Lett ; 101: 129652, 2024 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-38346577

RESUMO

Mixed-lineage protein kinase 3 (MLK3) is implicated in several human cancers and neurodegenerative diseases. A series of 3H-imidazo[4,5-b]pyridine derivatives were designed, synthesized and evaluated as novel MLK3 inhibitors. A homology model of MLK3 was developed and all designed compounds were docked to assess their binding pattern and affinity toward the MLK3 active site. Based on this knowledge, we synthesized and experimentally evaluated the designed compounds. Majority of the compounds showed significant inhibition of MLK3 in the enzymatic assay. In particular, compounds 9a, 9e, 9j, 9 k, 12b and 12d exhibited IC50 values of 6, 6, 8, 11, 14 and 14 nM, respectively. Furthermore, compounds 9a, 9e, 9 k and 12b exhibited favorable physicochemical properties among these compounds.


Assuntos
MAP Quinase Quinase Quinase 11 Ativada por Mitógeno , Piridinas , Humanos , Relação Estrutura-Atividade , Piridinas/química , Simulação de Acoplamento Molecular , Inibidores de Proteínas Quinases/química
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