Synthesis and activity evaluation of PARP-1 inhibitors with azaindole skeleton / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1792-1799, 2013.
Article
in Chinese
| 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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Aza Compounds
/
Chemistry
/
Poly(ADP-ribose) Polymerases
/
Poly (ADP-Ribose) Polymerase-1
/
Indoles
/
Metabolism
/
Antineoplastic Agents
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2013
Type:
Article
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