Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt.
Bioorg Med Chem Lett
; 27(9): 2047-2057, 2017 05 01.
Article
em En
| MEDLINE
| ID: mdl-28318945
ABSTRACT
A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity relationships and structure-based drug design methods led to the discovery of a series of modulators with improved RORγt inhibitory potency and inverse agonism properties.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Quinolinas
/
Desenho de Fármacos
/
Agonismo Inverso de Drogas
/
Membro 3 do Grupo F da Subfamília 1 de Receptores Nucleares
Tipo de estudo:
Diagnostic_studies
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2017
Tipo de documento:
Article