SAR156497, an exquisitely selective inhibitor of aurora kinases.
J Med Chem
; 58(1): 362-75, 2015 Jan 08.
Article
en En
| MEDLINE
| ID: mdl-25369539
ABSTRACT
The Aurora family of serine/threonine kinases is essential for mitosis. Their crucial role in cell cycle regulation and aberrant expression in a broad range of malignancies have been demonstrated and have prompted intensive search for small molecule Aurora inhibitors. Indeed, over 10 of them have reached the clinic as potential anticancer therapies. We report herein the discovery and optimization of a novel series of tricyclic molecules that has led to SAR156497, an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy. We also provide insights into its mode of binding to its target proteins, which could explain its selectivity.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Bencimidazoles
/
Quinolonas
/
Inhibidores de Proteínas Quinasas
/
Bibliotecas de Moléculas Pequeñas
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Aurora Quinasas
/
Antineoplásicos
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2015
Tipo del documento:
Article
País de afiliación:
Francia