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

作者：Ning, Chengqing; Huang, Wenyuan; Wu, Wen; Lu, Cheng; He, Yujun; Yao, Lei; Liu, Lifei; Zhen, Xiaohe; Liu, Xiaoyu^*; Yu, Niefang

来源：Letters in Drug Design and Discovery, 2015, 12(5): 344-350.

DOI：10.2174/1570180811666141024004832

• Antitumor
• cinnamic
• design
• histone deacetylase
• HDAC
• hydroxamaic acid

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.

• 出版日期2015
• 单位中南大学