Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation.
Bioorg Med Chem Lett
; 18(7): 2399-403, 2008 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-18337095
ABSTRACT
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 10nM to >20microM and were dependant upon both the nature of the aryl group and the tether joining the basic amine to the indolyl maleimide core of the inhibitors. Key interactions with the kinase ATP site and hinge region, predicted by homology modeling, were confirmed.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Derivados de Benzeno
/
Desenho de Fármacos
/
Inibidores Enzimáticos
/
Proteína Quinase Tipo 2 Dependente de Cálcio-Calmodulina
/
Indóis
/
Maleimidas
Tipo de estudo:
Prognostic_studies
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article