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The synthesis and biological evaluation of sanguinarine derivatives as anti-non-small cell lung cancer agents

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Abstract

A novel series of sanguinarine (SA) derivatives were synthesized and evaluated as anti-non-small cell lung cancer (NSCLC) agents. The compounds inhibited A549 and H1975 NSCLC cells with IC50 values of 0.96 – >30 μM and 0.79 – >30 μM, respectively. Compounds 8d–8j exhibited low micromolar inhibitory activity and indicated that the C6-position of SA was tolerated to be substituted by hydrophilic groups and CN. Further investigation of their mechanism of action showed that compound 8h induced apoptosis of A549 and H1975 cells by inhibiting the Akt signaling pathway and elevating the reactive oxygen species (ROS). This study provided a strategy for developing new anti-cancer agents.

Graphical abstract: The synthesis and biological evaluation of sanguinarine derivatives as anti-non-small cell lung cancer agents

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Article information


Submitted
20 Oct 2019
Accepted
19 Jan 2020
First published
12 Feb 2020

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

The synthesis and biological evaluation of sanguinarine derivatives as anti-non-small cell lung cancer agents

L. Jiang, X. Wang, Y. Wang, F. Xu, Z. Zhang, K. Ding and X. Lu, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/C9MD00494G

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