Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.
Bioorg Med Chem
; 19(4): 1550-61, 2011 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-21269836
ABSTRACT
Indoleamine 2,3-dioxygenase (IDO) is a heme dioxygenase which has been shown to be involved in the pathological immune escape of diseases such as cancer. The synthesis and structure-activity relationships (SAR) of a novel series of IDO inhibitors based on the indol-2-yl ethanone scaffold is described. In vitro and in vivo biological activities have been evaluated, leading to compounds with IC(50) values in the micromolar range in both tests. Introduction of small substituents in the 5- and 6-positions of the indole ring, indole N-methylation and variations of the aromatic side chain are all well tolerated. An iron coordinating group on the linker is a prerequisite for biological activity, thus corroborating the virtual screening results.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Indolamina-Pirrol 2,3,-Dioxigenase
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Etano
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Indóis
Limite:
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article