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

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

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

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Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 5 , 2015

DOI : 10.2174/1570180811666141024004832

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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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Letters in Drug Design & Discovery

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

VOLUME: 12 ISSUE: 5

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

Affiliation:School of Pharmaceutical Science, Central South University, Changsha, PR China.

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

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.

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Chengqing Ning, Wenyuan Huang, Wen Wu, Cheng Lu, Yujun He, Lei Yao, Lifei Liu, Xiaohe Zhen, Xiaoyu Liu and Niefang Yu, “Discovery of Novel HDAC Inhibitors by Structure-based Optimization of Cinnamic Hydroxamic Scaffold”, Letters in Drug Design & Discovery (2015) 12: 344. https://doi.org/10.2174/1570180811666141024004832

DOI https://doi.org/10.2174/1570180811666141024004832	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X

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VOLUME: 12
ISSUE: 5
Year: 2015

Published on: 24 March, 2015

Page: [344 - 350]
Pages: 7
DOI: 10.2174/1570180811666141024004832
Price: $65

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