Design, synthesis and anti-rheumatoid arthritis evaluation of double-ring conjugated enones.
Bioorg Chem
; 109: 104701, 2021 04.
Article
en En
| MEDLINE
| ID: mdl-33601137
ABSTRACT
Four series of double-ring conjugated enones were designed, synthesized and studied for the inhibition of synovial cell activity through the modification of Dysodensiol K core structure, double-ring, double-bond and double-carbonyl groups. For in vitro synovial cell assay of rats, compound 151 and 168 exhibited good inhibitory activities, with IC50 values of 2.71 ± 0.18 and 2.68 ± 0.16 µM respectively. At the same time, the LDH release and LD50 test results revealed that the target compounds were low cytotoxicity and acute toxicity. For in vivo CIA model test through the oral administration, compounds 151 and 168 were exhibited similar effect to positive control group methotrexate.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Diseño de Fármacos
/
Antirreumáticos
/
Annonaceae
Límite:
Animals
Idioma:
En
Revista:
Bioorg Chem
Año:
2021
Tipo del documento:
Article