Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells

作者：Zhang, Youjun; Ma, Hao; Wu, Yuelin; Wu, Zhongli; Yao, Zhengguang; Zhang, Wannian; Zhuang, Chunlin^*; Miao, Zhenyuan^*

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(11): 2308-2312.

DOI：10.1016/j.bmcl.2017.04.035

• Piperlongumine
• Natural product
• Drug design
• Structure-activity relationships
• Anticancer

Piperlongumine (PL) is a natural alkaloid with broad biological activities. Twelve analogues have been designed and synthesized with non-substituted benzyl rings or heterocycles in this work. Most of the compounds showed better anticancer activities than the parent PL without apparent toxicity in normal cells. Elevation of cellular ROS levels was one of the main anticancer mechanisms of these compounds. Cell apoptosis and cell cycle arrest for the best compound ZM90 were evaluated and similar mechanism of action with PL was demonstrated. The SAR was also characterized, providing worthy directions for further optimization of PL compounds.

• 出版日期2017-6-1
• 单位中国人民解放军第二军医大学; 上海应用技术大学; 宁夏医科大学