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

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

Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 5 , 2015

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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.

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Article Details

VOLUME: 12
ISSUE: 5
Year: 2015
Page: [344 - 350]
Pages: 7
DOI: 10.2174/1570180811666141024004832
Price: $58

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