Bioorganic and Medicinal Chemistry Letters p. 2308 - 2312 (2017)
Update date:2022-08-17
Topics:
Zhang, Youjun
Ma, Hao
Wu, Yuelin
Wu, Zhongli
Yao, Zhengguang
Zhang, Wannian
Zhuang, Chunlin
Miao, Zhenyuan
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.
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