Design, Synthesis and Activity of Benzofuran-7-carboxamide Poly(ADP-ribose)-polymerase Inhibitors

被引：4
作者：
Jin, Qiu [1 ,2 ]
Xin, Minhang [2 ]
Cong, Xin [2 ]
You, Qidong [1 ]
机构：
[1] China Pharmaceut Univ, Jiangsu Key Lab Drug Design & Optimizat, Nanjing 210009, Jiangsu, Peoples R China
[2] Jiangsu Simcere Pharmaceut Co Ltd, Jiangsu Key Lab Mol Targeted Antitumor Drug Res, Nanjing 210042, Jiangsu, Peoples R China
来源：
CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2013年 / 33卷 / 03期
基金：
美国国家科学基金会;
关键词：
PARP inhibitor; Benzofuran-7-carboxamide; anti-tumor; synthesis; PARP INHIBITORS; POLYMERASE; STRATEGY;
D O I：
10.6023/cjoc201211019
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Poly-(ADP-ribose)-polymerase (PARP) is a promising anti-cancer target as it plays a crucial role in the cellular reparation and survival mechanisms. A series of benzofuran-7-carboxamides was designed to maintain the required pharmacophore conformation through an intramolecular hydrogen bond. Twelve compounds were synthesized and the inhibitory effect on PARP activity of these compounds were tested and evaluated. The results showed that all the target compounds displayed potency against the PARP enzyme, and compound 7c was the most potent one with an IC50 value of 20.5 nmol.L-1.
引用
收藏
页码：590 / 595
页数：6
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