Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft.
Bioorg Med Chem Lett
; 25(22): 5163-7, 2015 Nov 15.
Article
en En
| MEDLINE
| ID: mdl-26463130
ABSTRACT
Selective estrogen receptor degraders (SERDs) have shown promise for the treatment of ER+ breast cancer. Disclosed herein is the continued optimization of our indazole series of SERDs. Exploration of ER degradation and antagonism in vitro followed by in vivo antagonism and oral exposure culminated in the discovery of indazoles 47 and 56, which induce tumor regression in a tamoxifen-resistant breast cancer xenograft.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Tamoxifeno
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Neoplasias de la Mama
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Antagonistas del Receptor de Estrógeno
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Indazoles
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Antineoplásicos
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2015
Tipo del documento:
Article