Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor.
Bioorg Med Chem
; 27(16): 3619-3631, 2019 08 15.
Article
en En
| MEDLINE
| ID: mdl-31279524
ABSTRACT
Twenty eight new aryloxybenzene analogues were synthesized and their in vitro binding potencies toward S1PR2 were determined using a [32P]S1P competitive binding assay. Out of these new analogues, three compounds, 28c (IC50â¯=â¯29.9⯱â¯3.9â¯nM), 28e (IC50â¯=â¯14.6⯱â¯1.5â¯nM), and 28g (IC50â¯=â¯38.5⯱â¯6.3â¯nM) exhibited high binding potency toward S1PR2 and high selectivity over the other four receptor subtypes (S1PR1, 3, 4, and 5; IC50â¯>â¯1000â¯nM). Each of the three potent compounds 28c, 28e, and 28g contains a fluorine atom that will allow to develop F-18 labeled PET radiotracers for imaging S1PR2.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Flúor
/
Receptores de Esfingosina-1-Fosfato
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2019
Tipo del documento:
Article
País de afiliación:
Estados Unidos