Design, synthesis, and cytotoxic activity of pyridine-based stilbenes

Abstract

In the present study, three series of 35 pyridine-based stilbenes include 10 new compounds prepared by Horner-Wadsworth-Emmons (HWE) reaction were assayed for cytotoxic activities toward two tumoral cell lines (K562 and MDA-MB-231) and one non-tumoral cell line (L-02). The bioassay results indicated that hybrid stilbenes formed at the C-3 position of pyridine displayed stronger antiproliferative activities against K562 cells and C-4 pyridine-based stilbenes showed broad-spectrum cytotoxic effects. Among them, C-3 pyridine-based stilbene PS2g bearing 2,6-dimethoxy possessed extremely potent antiproliferative activity with IC₅₀ values 1.46 µM against K562 cells, along with excellent selectivity towards normal L-02 cells. In summary, the present study contributes to the development of natural stilbene-based derivatives as antitumor agents and PS2g may serve as a promising lead for the treatment of chronic myeloid leukemia (CML) worthy further investigation.

Graphical Abstract

Keywords:

• Pyridine-based stilbene
• cytotoxicity
• CML

Acknowledgment

Special thanks are given to Jing Li (Ocean University of China) for the cytotoxic activity test.

Disclosure statement

No potential conflict of interest was reported by the authors.

Date availability statement

Data available within the article or its supplementary materials.

Additional information

Funding

This work was supported by the NSFC (Grant No. U2006204), the NSFC-TRF project (Grant No. 2181101213), the National Key Research and Development Program of China (2018YFC0310903).