Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).
Bioorg Med Chem Lett
; 21(18): 5633-7, 2011 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-21798738
ABSTRACT
A novel class of pyrazolopyrimidine-sulfonamides was discovered as selective dual inhibitors of aurora kinase A (AKA) and cyclin-dependent kinase 1 (CDK1). These inhibitors were originally designed based on an early lead (compound I). SAR development has led to the discovery of potent inhibitors with single digit nM IC(50)s towards both AKA and CDK1. An exemplary compound 1a has demonstrated good efficacy in an HCT116 colon cancer xenograft model.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
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Sulfonamidas
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Proteína Quinase CDC2
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Proteínas Serina-Treonina Quinases
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Neoplasias do Colo
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Inibidores de Proteínas Quinases
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Antineoplásicos
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article