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

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:

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.

Cite this article as:

Ning Chengqing, Huang Wenyuan, Wu Wen, Lu Cheng, He Yujun, Yao Lei, Liu Lifei, Zhen Xiaohe, Liu Xiaoyu and Yu Niefang, Discovery of Novel HDAC Inhibitors by Structure-based Optimization of Cinnamic Hydroxamic Scaffold, Letters in Drug Design & Discovery 2015; 12 (5) . https://dx.doi.org/10.2174/1570180811666141024004832