Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Bioorg Med Chem Lett
; 28(1): 15-23, 2018 01 01.
Article
em En
| MEDLINE
| ID: mdl-29169673
ABSTRACT
A novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP, compound 35 (GNE-207), has been identified through SAR investigations focused on optimizing al bicyclic heteroarene to replace the aniline present in the published GNE-272 series. Compound 35â¯has excellent CBP potency (CBP IC50â¯=â¯1â¯nM, MYC EC50â¯=â¯18â¯nM), a selectively index ofâ¯>2500-fold against BRD4(1), and exhibits a good pharmacokinetic profile.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Compostos de Bifenilo
/
Desenho de Fármacos
/
Fatores de Transcrição de p300-CBP
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article