Synthesis and structure-activity relationship of 2-arylamino-4-aryl-pyrimidines as potent PAK1 inhibitors.
Bioorg Med Chem Lett
; 23(14): 4072-5, 2013 Jul 15.
Article
em En
| MEDLINE
| ID: mdl-23756368
ABSTRACT
2-Arylamino-4-aryl-pyrimidines were found to be potent inhibitors of PAK1 kinase. The synthesis and SAR are described. The incorporation of a bromide at the 5-position of the pyrimidine core and in combination with a 1,2-dimethylpiperazine pendant domain yielded a lead compound with potent PAK1 inhibition and anti-proliferative activity in various colon cancer cell lines.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirimidinonas
/
Inibidores de Proteínas Quinases
/
Quinases Ativadas por p21
/
Compostos de Anilina
Limite:
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article