2. Academic Validation
  3. Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells

Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells

  • Bioorg Med Chem Lett. 2017 Jun 1;27(11):2308-2312. doi: 10.1016/j.bmcl.2017.04.035.
Youjun Zhang 1,  Hao Ma 2,  Yuelin Wu 3,  Zhongli Wu 1,  Zhengguang Yao 4,  Wannian Zhang 2,  Chunlin Zhuang 5,  Zhenyuan Miao 6
Affiliations

Affiliations

  • 1 Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China.
  • 2 Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China; Ningxia Medical University, Yinchuan 750004, China.
  • 3 Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418, China.
  • 4 Ningxia Medical University, Yinchuan 750004, China.
  • 5 Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China. Electronic address: zclnathan@163.com.
  • 6 Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China. Electronic address: miaozhenyuan@hotmail.com.
PMID: 28434764 DOI: 10.1016/j.bmcl.2017.04.035
Abstract

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.

Keywords

Anticancer; Drug design; Natural product; Piperlongumine; Structure-activity relationships.

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