Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.
Bioorg Med Chem Lett
; 27(3): 582-585, 2017 02 01.
Article
em En
| MEDLINE
| ID: mdl-28003141
ABSTRACT
The discovery of a series of structurally-novel biaryl urea IDO inhibitors is described. Optimization of a micromolar hit through iterative cycles of synthesis and screening in an assay measuring IDO-mediated intracellular conversion of tryptophan to kynurenine led to potent inhibitors with favorable selectivity and metabolic stability profiles.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ureia
/
Ácidos Carboxílicos
/
Inibidores Enzimáticos
/
Indolamina-Pirrol 2,3,-Dioxigenase
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2017
Tipo de documento:
Article