Discovery and optimization of novel benzothiophene-3-carboxamides as highly potent inhibitors of Aurora kinases A and B.
Bioorg Med Chem Lett
; 28(19): 3265-3270, 2018 10 15.
Article
em En
| MEDLINE
| ID: mdl-30143423
ABSTRACT
Aurora kinases as regulators of cell division have become promising therapeutic targets recently. Here we report novel, low molecular weight benzothiophene-3-carboxamide derivatives designed and optimized for inhibiting Aurora kinases. The most effective compound 36 inhibits Aurora kinases in vitro in the nanomolar range and diminishes HCT 116 cell viability blocking cytokinesis and inducing apoptosis. According to western blot analysis, the lead molecule inhibits Aurora kinases equipotently to VX-680 (Tozasertib) and similarly synergizes with other targeted drugs.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Tiofenos
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Inibidores de Proteínas Quinases
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Aurora Quinase A
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Aurora Quinase B
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Amidas
Limite:
Humans
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article