Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.
Bioorg Med Chem Lett
; 18(20): 5618-21, 2008 Oct 15.
Article
en En
| MEDLINE
| ID: mdl-18793846
ABSTRACT
A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src kinase family. Highly efficient parallel syntheses were devised to prepare analogues for SAR studies. A number of these 4-amino-6-benzimidazole-pyrimidines exhibited single-digit nanomolar IC(50)s against Lck in biochemical and cellular assays. These 4-amino-6-benzimidazole-pyrimidines represent a new class of tyrosine kinase inhibitors.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Pirimidinas
/
Bencimidazoles
/
Química Farmacéutica
/
Proteína Tirosina Quinasa p56(lck) Específica de Linfocito
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2008
Tipo del documento:
Article
País de afiliación:
Estados Unidos