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Medicinal Chemistry Research

, Volume 26, Issue 11, pp 2879–2888 | Cite as

Design, synthesis and biological evaluation of urea-based benzamides derivatives as HDAC inhibitors

  • Yong Zhu
  • Xin Chen
  • Ting Ran
  • Jiaqi Niu
  • Shuang Zhao
  • Tao Lu
  • Weifang Tang
Original Research
  • 249 Downloads

Abstract

A new class of urea-based benzamides derivatives were designed and synthesized as histone deacetylases inhibitors. Biological evaluations of these compounds included the inhibitory activity of histone deacetylases1 and cytotoxicity against different cancer cell lines in vitro. Most compounds exhibited potential histone deacetylases inhibitory activity and antitumor activities. Compound 5h behaved as potent histone deacetylases1 inhibitor (IC50 = 0.182 μM) and showed comparable cytotoxicity with MS-275, which could be considered as a potential candidate compound for further development.

Keywords

Benzamides derivatives HDAC inhibitors Design Synthesis 

Notes

Acknowledgements

This study was supported by the National Natural Science Foundation of China (Grant No. 81202410), Research Fund for the Doctoral Program of Higher Education of China (Grant No. 20120096120010) and Fundamental Research Funds for the Central Universities (Grant No. JKPZ2013003).

Compliance with ethical standards

Conflict of interest

The authors declare that they have no competing interests.

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Copyright information

© Springer Science+Business Media, LLC 2017

Authors and Affiliations

  • Yong Zhu
    • 1
  • Xin Chen
    • 1
  • Ting Ran
    • 2
  • Jiaqi Niu
    • 1
  • Shuang Zhao
    • 1
  • Tao Lu
    • 1
    • 3
  • Weifang Tang
    • 1
  1. 1.Department of Organic Chemistry, School of ScienceChina Pharmaceutical UniversityNanjing,China
  2. 2.Laboratory of Molecular Design and Drug Discovery, School of ScienceChina Pharmaceutical UniversityNanjing,China
  3. 3.State Key laboratory of Natural MedicinesChina Pharmaceutical UniversityNanjing,China

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