Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

Back

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.

Graphical Abstract:


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.

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

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