Insights into the myosin II inhibitory potency of A-ring-modified (S)-blebbistatin analogs.
Bioorg Med Chem Lett
; 27(13): 2986-2989, 2017 07 01.
Article
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| MEDLINE
| ID: mdl-28512027
ABSTRACT
Myosin II is an interesting target for therapeutic intervention, as it is involved in a large number of motility-based diseases. (S)-Blebbistatin is a known micromolar inhibitor of this protein. A new series of (S)-blebbistatin derivatives with a modified A-ring was synthesized and the myosin II inhibitory properties were evaluated in vitro. In this way, we gained insight into the influence of structural modifications in this part of the scaffold on myosin II inhibitory potency. Our results indicate there are few possibilities for potency enhancement via ring A modification of the blebbistatin scaffold.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Miosina Tipo II
/
Dictyostelium
/
Inhibidores Enzimáticos
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Compuestos Heterocíclicos de 4 o más Anillos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2017
Tipo del documento:
Article
País de afiliación:
Bélgica