Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
Bioorg Med Chem
; 26(3): 590-602, 2018 02 01.
Article
en En
| MEDLINE
| ID: mdl-29289448
ABSTRACT
Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Quinasa Idelta de la Caseína
/
Caseína Cinasa 1 épsilon
/
Inhibidores de Proteínas Quinasas
Límite:
Animals
/
Female
/
Humans
/
Male
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2018
Tipo del documento:
Article
País de afiliación:
Estados Unidos