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Letters in Drug Design & Discovery

Author(s): Chengqing Ning, Wenyuan Huang, Wen Wu, Cheng Lu, Yujun He, Lei Yao, Lifei Liu, Xiaohe Zhen, Xiaoyu Liu and Niefang Yu

DOI: 10.2174/1570180811666141024004832

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Discovery of Novel HDAC Inhibitors by Structure-based Optimization of Cinnamic Hydroxamic Scaffold

Page: [344 - 350] Pages: 7

  • * (Excluding Mailing and Handling)

Abstract

A series of di-substituted cinnamic hydroxamic derivatives was designed, synthesized and evaluated as HDAC inhibitors. Compound 5f (HS270) demonstrated potent HDAC inhibitory and antiproliferative activities. In xenograft model, 5f showed significant antitumor efficacy in tumorbearing mice.

Keywords: Antitumor, cinnamic, design, histone deacetylase, HDAC, hydroxamaic acid.

Graphical Abstract