1.
Assay Drug Dev Technol
; 13(4): 185, 2015 May.
Artigo
em Inglês
| MEDLINE
| ID: mdl-26065555
2.
Bioorg Med Chem Lett
; 25(9): 1842-8, 2015 May 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-25851940
RESUMO
In this report we detail the evolution of our previously reported thiophene isoxazole BET inhibitor chemotype exemplified by CPI-3 to a novel bromodomain selective chemotype (the methyl isoxazoleazepine chemotype) exemplified by carboxamide 23. The methyl isoxazoleazepine chemotype provides potent inhibition of the bromodomains of the BET family, excellent in vivo PK across species, low unbound clearance, and target engagement in a MYC PK-PD model.
