Benzofuran derivatives as a novel class of inhibitors of mTOR signaling.
Eur J Med Chem
; 74: 41-9, 2014 Mar 03.
Article
em En
| MEDLINE
| ID: mdl-24445311
ABSTRACT
High-throughput screening (HTS) hit 1 was previously identified as an inhibitor of the Akt/mTOR (Akt/mammalian target of rapamycin) signaling, which is a major target in oncology. The cytotoxicity of 1 was determined on a panel of human cancer cells lines with an IC50 comprised between 30 and 140 µM. Subsequent structure--activity relationship (SAR) studies led us to the identification of compounds that displayed an enhanced cytotoxicity. We demonstrated also that these molecules directly bind to mTOR complex 1 (mTORC1) and inhibit its kinase activity.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzofuranos
/
Transdução de Sinais
/
Serina-Treonina Quinases TOR
Limite:
Humans
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
França