Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors.
Bioorg Med Chem Lett
; 19(23): 6784-7, 2009 Dec 01.
Article
em En
| MEDLINE
| ID: mdl-19836232
ABSTRACT
A series of deoxycytidine kinase inhibitors was simultaneously optimized for potency and PK properties. A co-crystal structure then allowed merging this series with a high throughput screening hit to afford a highly potent, selective and orally bioavailable inhibitor, compound 10. This compound showed dose dependent inhibition of deoxycytidine kinase in vivo.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
/
Desoxicitidina
/
Desoxicitidina Quinase
/
Inibidores de Proteínas Quinases
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2009
Tipo de documento:
Article
País de afiliação:
Estados Unidos