Synthesis and activity evaluation of PARP-1 inhibitors with azaindole skeleton / 药学学报
Acta Pharmaceutica Sinica
; (12): 1792-9, 2013.
Article
en Zh
| WPRIM
| ID: wpr-448789
Biblioteca responsable:
WPRO
ABSTRACT
PARP [poly(ADP-ribose)polymerase] represents a novel potential target in cancer therapy. It is involved in a DNA repair process by catalyzing the transfer of ADP-ribose units from NAD to a number of its substrate proteins. In this work, a series of novel azaindole derivatives was designed and synthesized. Moreover, 16 target molecules were screened and 8 compounds displayed inhibitory activity against PARP-1. It has been demonstrated that these azaindoles bearing cycloamine substituents at 2-position were active to both PARP-1 and PARP-2.
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1
Base de datos:
WPRIM
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2013
Tipo del documento:
Article