Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design.
Bioorg Med Chem Lett
; 16(12): 3310-4, 2006 Jun 15.
Article
em En
| MEDLINE
| ID: mdl-16600594
ABSTRACT
Guided by structure-based drug design, modification of the 1,4-benzodiazepin-2,5-dione lead compound 1 resulted in the discovery of 19, a potent and orally bioavailable antagonist of the HDM2-p53 protein-protein interaction (FP IC50 = 0.7 microM, F approximately 100%).
Buscar no Google
Base de dados:
MEDLINE
Assunto principal:
Benzodiazepinas
/
Desenho de Fármacos
/
Proteína Supressora de Tumor p53
/
Proteínas Proto-Oncogênicas c-mdm2
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article