Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties.
J Med Chem
; 46(5): 876-9, 2003 Feb 27.
Article
en En
| MEDLINE
| ID: mdl-12593668
ABSTRACT
The first series of synthetic 1-aza-9-oxafluorenes with cytostatic activities in the micromolar range was evaluated as cyclin-dependent kinase (CDK1) inhibitors. Activity was found to be selective in comparison to the inhibition of other kinases within the CDK family. Compounds were shown to inhibit the membrane-efflux pump P-glycoprotein responsible for multidrug resistance in cancer cells. First structure-activity relationships are discussed.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Compuestos Aza
/
Proteína Quinasa CDC2
/
Subfamilia B de Transportador de Casetes de Unión a ATP
/
Fluorenos
/
Sustancias Intercalantes
/
Antineoplásicos
Límite:
Animals
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2003
Tipo del documento:
Article
País de afiliación:
Alemania