2. Academic Validation
  3. Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol

Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol

  • Bioorg Med Chem Lett. 2017 Mar 1;27(5):1325-1328. doi: 10.1016/j.bmcl.2016.08.016.
Xiaojuan Xu 1,  Xia Fang 2,  Jun Wang 2,  Hong Zhu 2
Affiliations

Affiliations

  • 1 School of Chemistry and Chemical Engineering, Yancheng Teachers University, Yancheng, China. Electronic address: xxjyctu@163.com.
  • 2 School of Chemistry and Chemical Engineering, Yancheng Teachers University, Yancheng, China.
PMID: 28159415 DOI: 10.1016/j.bmcl.2016.08.016
Abstract

A series of novel ROS inducers were designed by merging the fragments of piperlongumine and dicoumarol. Most of these derivatives showed potent in vitro activity against three Cancer cell lines and good selectivity towards normal lung cells. The most potent and selective compound 3e was proven to exhibit obvious ROS elevation and excellent in vivo antitumor activity with suppressed tumor growth by 48.46% at the dose of 5mg/kg. Supported by these investigation, these findings encourage further investigation around this interesting antitumor chemotype.

Keywords

Antitumor; Biological activity; Dicoumarol; Piperlongumine; Reactive oxygen species.

Figures