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Chinese Journal of Organic Chemistry >

2013 , Vol. 33 >Issue 03: 590 - 595

DOI: https://doi.org/10.6023/cjoc201211019

Articles

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

  • Jin Qiu ,
  • Xin Minhang ,
  • Cong Xin ,
  • You Qidong
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  • a Jiangsu Key Laboratory of Drug Design & Optimization, China Pharmaceutical University, Nanjing 210009;
    b Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research, Jiangsu Simcere Pharmaceutical Co., Ltd., Nanjing 210042

Received date: 2012-11-09

  Revised date: 2012-12-03

  Online published: 2012-12-06

Supported by

Project supported by the National Science Foundation of Jiangsu Province (No. BK2011086).

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Abstract

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稬-1.

Key words： PARP inhibitor; Benzofuran-7-carboxamide; anti-tumor; synthesis

Cite this article

Jin Qiu , Xin Minhang , Cong Xin , You Qidong . Design, Synthesis and Activity of Benzofuran-7-carboxamide Poly(ADP-ribose)-polymerase Inhibitors[J]. Chinese Journal of Organic Chemistry, 2013 , 33(03) : 590 -595 . DOI: 10.6023/cjoc201211019

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