1.
Bioorg Med Chem Lett
; 25(9): 1905-9, 2015 May 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-25857941
RESUMEN
This Letter describes synthesis, SAR, and biological activity of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides as inhibitors of γ-secretase mediated signaling of Notch receptors. Optimization of this series led to the identification of BMS-871 (compound 30) which displayed robust in vivo efficacy in Notch-dependent leukemia and solid tumor xenograft models.