Inhibition of ALK2 with bicyclic pyridyllactams.
Bioorg Med Chem Lett
; 55: 128452, 2022 01 01.
Article
em En
| MEDLINE
| ID: mdl-34780900
ABSTRACT
Activin receptor-like kinase 2 (ALK2) has been implicated as a key target in multiple rare diseases. Herein, we describe the design of a novel bicyclic lactam series of potent and selective ALK2 inhibitors. This manuscript details an improvement in potency of two orders of magnitude from the initial bicyclic structure as well as a two-fold improvement in cellular potency from the original monocyclic inhibitor. Furthermore, we provide a detailed strategy for progressing this project in the future.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores de Ativinas Tipo I
/
Beta-Lactamas
/
Inibidores de Proteínas Quinases
Limite:
Humans
Idioma:
En
Ano de publicação:
2022
Tipo de documento:
Article