Synthesis and activity evaluation of PARP-1 inhibitors with azaindole skeleton / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1792-1799, 2013.
Artigo
em Chinês
| WPRIM
| ID: wpr-298009
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.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Compostos Aza
/
Química
/
Poli(ADP-Ribose) Polimerases
/
Poli(ADP-Ribose) Polimerase-1
/
Indóis
/
Metabolismo
/
Antineoplásicos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2013
Tipo de documento:
Artigo
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