Studies on Benzofuran-7-carboxamides as Poly(ADP-ribose) Polymerase-1 (PARP-1) Inhibitors

Bulletin of the Korean chemical society

Kyu Yang Yi¹  Byung Ho Lee¹  Sunkyung Lee¹   Kwang Seok Oh¹ 

关键词: Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor;    Benzofuran-7-carboxamide;    Nicotinamide;    Anticancer;    Ischemic disease;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

Benzofuran-7-carboxamide was identified as a novel scaffold of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. A series of compounds with various 2-substituents including (tertiary amino)methyl moieties substituted with aryl ring and aryl groups containing tertiary amines, were synthesized and biologically evaluated to elucidate the structure-activity relationships and optimize the potency. 2-[4-(Pyrrolidin-1-ylmethyl)phenyl]- benzofuran-7-carboxamide (42) was the most potent as an IC50 value of 40 nM among those.

【 授权许可】

Unknown