1.
ACS Med Chem Lett
; 4(9): 835-40, 2013 Sep 12.
Artigo
em Inglês
| MEDLINE
| ID: mdl-24900758
RESUMO
The identification of a novel series of small molecule BET inhibitors is described. Using crystallographic binding modes of an amino-isoxazole fragment and known BET inhibitors, a structure-based drug design effort lead to a novel isoxazole azepine scaffold. This scaffold showed good potency in biochemical and cellular assays and oral activity in an in vivo model of BET inhibition.