[Synthesis and activity evaluation of PARP-1 inhibitors with azaindole skeleton].
Yao Xue Xue Bao
; 48(12): 1792-9, 2013 Dec.
Article
em Zh
| MEDLINE
| ID: mdl-24689236
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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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Aza
/
Indóis
/
Antineoplásicos
Idioma:
Zh
Ano de publicação:
2013
Tipo de documento:
Article