Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II.
Bioorg Med Chem Lett
; 19(23): 6613-7, 2009 Dec 01.
Article
em En
| MEDLINE
| ID: mdl-19854650
ABSTRACT
C-6 Biarylmethylamino purine derivatives of roscovitine (1) inhibit cyclin dependent kinases and demonstrate potent antiproliferative activity. Replacement of the aryl rings of the C-6 biarylmethylamino group with heterobiaryl rings has provided compounds with significantly improved activity. In particular, derivatives 18 g and 9 c demonstrated 1000-fold and 1250-fold improvements, respectively, in the growth inhibition of HeLa cells compared to roscovitine (1).
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Purinas
/
Quinases Ciclina-Dependentes
/
Inibidores de Proteínas Quinases
/
Antineoplásicos
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article