Synthesis and activity evaluation of PARP-1 inhibitors with azaindole skeleton.
- Author:
Jie ZHOU
;
Zhi-Xiang ZHU
;
Xiao-Guang CHEN
;
Bai-Ling XU
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Aza Compounds;
chemical synthesis;
chemistry;
pharmacology;
Indoles;
chemical synthesis;
chemistry;
pharmacology;
Poly (ADP-Ribose) Polymerase-1;
Poly(ADP-ribose) Polymerases;
metabolism
- From:
Acta Pharmaceutica Sinica
2013;48(12):1792-1799
- CountryChina
- Language:Chinese
-
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.
