5-Aryl-furan derivatives bearing a phenylalanine- or isoleucine-derived rhodanine moiety as potential PTP1B inhibitors.
Bioorg Chem
; 106: 104483, 2021 01.
Article
em En
| MEDLINE
| ID: mdl-33268007
ABSTRACT
Two series of 5-aryl-furan derivatives bearing a phenylalanine- or isoleucine-derived rhodanine moiety were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, 5g was found to have the best PTP1B inhibitory potency (IC50 = 2.66 ± 0.16 µM) and the best cell division cycle 25 homolog B (CDC25B) inhibitory potency (IC50 = 0.25 ± 0.02 µM). Enzymatic data together with molecular modeling results demonstrated that the introduction of a sec-butyl group at the 2-position of the carboxyl group remarkably improved the PTP1B inhibitory activity.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Fenilalanina
/
Rodanina
/
Inibidores Enzimáticos
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Proteína Tirosina Fosfatase não Receptora Tipo 1
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Furanos
/
Isoleucina
Limite:
Humans
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article