Chelate oxorhenium to assemble new integrin antagonists.
J Inorg Biochem
; 105(6): 880-6, 2011 Jun.
Article
em En
| MEDLINE
| ID: mdl-21510913
ABSTRACT
Assembly of independent chemical modules through oxorhenium coordination by a NS(2)+S chelation motif was applied to the synthesis of RGD (Arg-Gly-Asp) analogs. Modules were assembled through oxorhenium chelation to give a series of 18 metal complexes in good yields and satisfactory purities. Screening of these oxorhenium coordinates as antagonists of integrins αVß3, αIIbß3 and αVß5 led to the identification of 3 bioactive compounds that exhibit submicromolar affinities for the 3 integrins. Preliminary studies showed that the corresponding oxotechnetium complexes are stable in mice plasma and therefore could be proposed for the molecular imaging of pathologies that overexpress integrins αVß3 and αVß5.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Rênio
/
Integrinas
/
Quelantes
Limite:
Animals
Idioma:
En
Revista:
J Inorg Biochem
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
França