Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao, China.
Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology, Qingdao, China.
Nat Prod Res. 2024 Jun;38(11):1961-1966. doi: 10.1080/14786419.2023.2227991. Epub 2023 Jun 29.
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 bearing 2,6-dimethoxy possessed extremely potent antiproliferative activity with IC 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 may serve as a promising lead for the treatment of chronic myeloid leukemia (CML) worthy further investigation.
在本研究中，三组 35 个吡啶二苯乙烯类化合物，包括通过 Horner-Wadsworth-Emmons（HWE）反应制备的 10 个新化合物，针对两种肿瘤细胞系（K562 和 MDA-MB-231）和一种非肿瘤细胞系（L-02）进行了细胞毒性活性测试。生物测定结果表明，在吡啶的 C-3 位形成的杂化二苯乙烯对 K562 细胞显示出更强的抗增殖活性，而 C-4 位的吡啶二苯乙烯具有广谱的细胞毒性作用。其中，具有 2,6-二甲氧基的 C-3 位吡啶二苯乙烯对 K562 细胞具有极其强大的抗增殖活性，IC 值为 1.46 μM，对正常 L-02 细胞具有优异的选择性。总之，本研究为开发基于天然二苯乙烯的衍生物作为抗肿瘤剂做出了贡献，可能为治疗慢性髓性白血病（CML）提供有前途的先导化合物，值得进一步研究。
