A one-pot efficient, practical and eco-friendly synthesis of tocopherol analogues has been developed using water or solvent free conditions via Passerini and Ugi multicomponent reactions. These reactions can be optimized using microwave irradiation or ultrasound as the energy source. Accordingly, a small library of 30 compounds was prepared for biological tests. The evaluation of the antiproliferative activity in the human solid tumor cell lines A549 (lung), HBL-100 (breast), HeLa (cervix), SW1573 (lung), T-47D (breast), and WiDr (colon) provided lead compounds with GI₅₀ values between 1 and 5 μM. A structure–activity relationship is also discussed. One of the studied compounds comes up as a future candidate for the development of potent tocopherol-mimetic therapeutic agents for cancer.

通过Passerini和Ugi多组分反应，在无水或无溶剂条件下，开发了一种一锅高效，实用且环保的生育酚类似物合成方法。可以使用微波辐射或超声波作为能源来优化这些反应。因此，准备了一个包含30种化合物的小型文库用于生物学测试。对人实体瘤细胞系A549（肺），HBL-100（乳腺），HeLa（子宫颈），SW1573（肺），T-47D（乳腺）和WiDr（结肠）的抗增殖活性的评估提供了先导化合物带有GI ₅₀值介于1和5μM之间。还讨论了结构与活动的关系。研究的化合物之一有望成为开发有效的模拟生育酚的癌症治疗药物的未来候选者。