Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
Bioorg Med Chem Lett
; 15(7): 1895-9, 2005 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-15780629
ABSTRACT
Tetrahydroquinoline-based small molecule inhibitors of farnesyltransferase (FT) have been identified. Lead compounds were shown to have nanomolar to sub-nanomolar activity in biochemical assays with excellent potency in a Ras-mutated cellular reversion assay. BMS-316810 (9e), a 0.7 nM FT inhibitor, was orally-active in a nude mouse tumor allograft efficacy study.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Quinolinas
/
Alquil e Aril Transferases
/
Inibidores Enzimáticos
/
Antineoplásicos
Limite:
Animals
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article