Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, Italy.
Department of Science, University of Basilicata, Viale dell'Ateneo Lucano 10, 85100 Potenza, Italy.
Int J Mol Sci. 2020 Oct 21;21(20):7797. doi: 10.3390/ijms21207797.
Breast cancer represents the most frequently diagnosed malignancy in women worldwide. Various therapeutics are currently used in order to halt the progression of breast tumor, even though certain side effects may limit the beneficial effects. In recent years, many efforts have been addressed to the usefulness of natural compounds as anticancer agents due to their low toxicity. Resveratrol, a stilbene found in grapes, berries, peanuts and soybeans, has raised a notable interest for its antioxidant, anti-inflammatory, and antitumor properties. Here, we report the design, the synthesis and the characterization of the anticancer activity of a small series of imino -aryl-substituted compounds that are analogues of resveratrol. In particular, the most active compound, named , exhibited anti-tumor activity in diverse types of breast cancer cells through the inhibition of the human topoisomerase II and the induction of apoptotic cell death. Therefore, the abovementioned compound maybe considered as a promising agent in more comprehensive treatments of breast cancer.
乳腺癌是全球女性最常见的恶性肿瘤。目前有多种治疗方法用于阻止乳腺癌肿瘤的进展，尽管某些副作用可能会限制其有益作用。近年来，由于天然化合物的低毒性，人们越来越关注其作为抗癌药物的用途。白藜芦醇是一种存在于葡萄、浆果、花生和大豆中的芪类化合物，因其具有抗氧化、抗炎和抗肿瘤特性而引起了人们的极大兴趣。在这里，我们报告了一系列亚氨基芳基取代化合物的设计、合成和抗癌活性的研究，这些化合物是白藜芦醇的类似物。特别是，名为 的最活性化合物通过抑制人拓扑异构酶 II 和诱导细胞凋亡性死亡，在多种类型的乳腺癌细胞中表现出抗肿瘤活性。因此，上述化合物可被视为更全面治疗乳腺癌的有前途的药物。
