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

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 ?M and 0.79 - >30 ?M, 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.

SUBMITTER: Jiang L

PROVIDER: S-EPMC7489057 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature

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

Jiang Liang L Wang Xiaolu X Wang Yuting Y Xu Fang F Zhang Zhang Z Ding Ke K Lu Xiaoyun X

RSC medicinal chemistry 20200212 2

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 IC<sub>50</sub> values of 0.96 - >30 μM and 0.79 - >30 μM, respectively. Compounds <b>8d-8j</b> 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 compoun ...[more]

PMID: 33479636

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