2-Aminobenzimidazoles as potent Aurora kinase inhibitors.
Bioorg Med Chem Lett
; 19(17): 5158-61, 2009 Sep 01.
Article
en En
| MEDLINE
| ID: mdl-19646866
ABSTRACT
This Letter describes the discovery and key structure-activity relationship (SAR) of a series of 2-aminobenzimidazoles as potent Aurora kinase inhibitors. 2-Aminobenzimidazole serves as a bioisostere of the biaryl urea residue of SNS-314 (1c), which is a potent Aurora kinase inhibitor and entered clinical testing in patients with solid tumors. Compared to SNS-314, this series of compounds offers better aqueous solubility while retaining comparable in vitro potency in biochemical and cell-based assays; in particular, 6m has also demonstrated a comparable mouse iv PK profile to SNS-314.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Bencimidazoles
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Proteínas Serina-Treonina Quinasas
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Inhibidores de Proteínas Quinasas
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Antineoplásicos
Límite:
Animals
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Humans
Idioma:
En
Año:
2009
Tipo del documento:
Article