Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2).
Bioorg Med Chem Lett
; 24(24): 5801-5804, 2014 Dec 15.
Article
en En
| MEDLINE
| ID: mdl-25454272
ABSTRACT
As ENT inhibitors including dilazep have shown efficacy improving oHSV1 targeted oncolytic cancer therapy, a series of dilazep analogues was synthesized and biologically evaluated to examine both ENT1 and ENT2 inhibition. The central diamine core, alkyl chains, ester linkage and substituents on the phenyl ring were all varied. Compounds were screened against ENT1 and ENT2 using a radio-ligand cell-based assay. Dilazep and analogues with minor structural changes are potent and selective ENT1 inhibitors. No selective ENT2 inhibitors were found, although some analogues were more potent against ENT2 than the parent dilazep.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Tranportador Equilibrativo 1 de Nucleósido
/
Transportador Equilibrativo 2 de Nucleósido
/
Dilazep
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2014
Tipo del documento:
Article
País de afiliación:
Estados Unidos