Department of Pharmacy, Health and Nutrition Sciences, University of Calabria, 87036 Arcavacata di Rende, Cosenza, Italy.
Bioorg Med Chem Lett. 2013 Dec 1;23(23):6401-5. doi: 10.1016/j.bmcl.2013.09.054. Epub 2013 Sep 25.
Resveratrol (3,4',5 tri-hydroxystilbene), a natural plant polyphenol, has gained interest as a non-toxic agent capable of inducing tumor cell death in a variety of cancer types. However, therapeutic application of these beneficial effects remains very limited due to its short biological half-life, labile properties, rapid metabolism and elimination. Different studies were undertaken to obtain synthetic analogs of resveratrol with major bioavailability and anticancer activity. We have synthesized a series 3-chloro-azetidin-2-one derivatives, in which an azetidinone nucleus connects two aromatic rings. Aim of the present study was to investigate the effects of these new 3-chloro-azetidin-2-one resveratrol derivatives on human breast cancer cell lines proliferation. Our results indicate that some azetidin-based resveratrol derivatives may become new potent alternative tools for the treatment of human breast cancer.
白藜芦醇（3,4',5-三羟基二苯乙烯），一种天然植物多酚，作为一种能够诱导多种癌症类型肿瘤细胞死亡的无毒剂，已引起人们的关注。然而，由于其生物半衰期短、不稳定、代谢和消除迅速，这些有益作用的治疗应用仍然非常有限。进行了不同的研究以获得具有主要生物利用度和抗癌活性的白藜芦醇合成类似物。我们已经合成了一系列 3-氯-氮杂环丁烷-2-酮衍生物，其中氮杂环丁烷核连接两个芳环。本研究的目的是研究这些新的 3-氯-氮杂环丁烷-2-酮白藜芦醇衍生物对人乳腺癌细胞系增殖的影响。我们的结果表明，一些基于氮杂环丁烷的白藜芦醇衍生物可能成为治疗人类乳腺癌的新的有效替代工具。
