Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1alpha prolyl hydroxylase inhibitors.
Bioorg Med Chem Lett
; 16(21): 5517-22, 2006 Nov 01.
Article
em En
| MEDLINE
| ID: mdl-16931007
ABSTRACT
A new series of potent 8-hydroxyquinolines was designed based on the newly resolved X-ray crystal structure of EGLN-1. Both alkyl and aryl 8-hydroxyquinoline-7-carboxyamides were good HIF-1alpha prolyl hydroxylase (EGLN) inhibitors. In subsequent VEGF induction assays, these exhibited potent VEGF activity. In addition, this class of compounds did show the ability to stabilize HIF-1alpha.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
/
Oxiquinolina
/
Pró-Colágeno-Prolina Dioxigenase
Tipo de estudo:
Prognostic_studies
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article