Triaryl (Z)-olefins suitable for radiolabeling with carbon-11 or fluorine-18 radionuclides for positron emission tomography imaging of cyclooxygenase-2 expression in pathological disease.
Bioorg Med Chem Lett
; 20(17): 5245-50, 2010 Sep 01.
Article
en En
| MEDLINE
| ID: mdl-20655211
ABSTRACT
A group of (Z)-1,1-diphenyl-2-(4-methylsulfonylphenyl)alk-1-enes were synthesized using methodologies that will allow incorporation of a [(11)C]OCH(3) substituent at the para-position of the C-1 phenyl ring, a [(11)C]SO(2)CH(3) substituent at the para-position of the C-2 phenyl ring, a [(18)F]OCH(2)CH(2)F substituent at the para-position of the C-1 phenyl ring, and a [(18)F]CH(2)CH(2)F substituent at the C-2 position of the olefinic bond. The [(11)C] and [(18)F] radiotracers are designed as potential radiopharmaceuticals to image cyclooxygenase-2 (COX-2) expression in any organ where COX-2 is upregulated. The COX-1/COX-2 inhibition data acquired suggest that compounds having a [(11)C]OMe or [(18)F]OCH(2)CH(2)F substituent at the para-position of the C-1 phenyl ring may be more suitable for imaging COX-2 expression in view of their ability to exclusively inhibit the COX-2 isozyme.
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Radioisótopos de Carbono
/
Radioisótopos de Flúor
/
Enfermedad
/
Tomografía de Emisión de Positrones
/
Alquenos
/
Ciclooxigenasa 2
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Canadá