Kubiak Jakub, Szyk Piotr, Czarczynska-Goslinska Beata, Goslinski Tomasz
Chair and Department of Chemical Technology of Drugs, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznan, Poland.
Doctoral School, Poznan University of Medical Sciences, Bukowska 70, 60-812 Poznan, Poland.
Molecules. 2025 May 30;30(11):2395. doi: 10.3390/molecules30112395.
Flavonoids and chalcones, widely recognised for their diverse biological activities, have garnered attention due to their potential therapeutic applications. This review discusses fluorinated flavonoids and chalcones, focusing on their prospective anti-inflammatory, antidiabetic, anticancer, antiosteoporotic, cardioprotective, neuroprotective, hepatoprotective, antimicrobial, and antiparasitic applications. The enhanced biological activities of fluorinated derivatives, particularly the antibacterial, antiviral, and anticancer properties, are attributed to the introduction of fluorine groups, which increase lipophilicity and metabolic stability. Key findings indicate that fluorinated flavonoids and chalcones exhibit synergistic effects with antibiotics, inhibit bacterial efflux pumps, and reveal potent antiviral and anticancer properties. However, challenges such as cytotoxicity and structural optimisation have to be addressed. The synthesis of fluorinated flavonoids and chalcones is discussed, with emphasis on various synthetic methods such as condensation and cyclisation reactions starting from fluorinated precursors, as well as fluorination strategies, including the use of molecular fluorine or fluorinating agents. Fluorinated flavonoids and chalcones represent candidates for therapeutic development and have the potential to overcome drug resistance. However, further studies are necessary to adjust their pharmacological profiles.
黄酮类化合物和查耳酮因其多样的生物活性而广为人知，由于其潜在的治疗应用而受到关注。本综述讨论了氟化黄酮类化合物和查耳酮，重点关注它们在抗炎、抗糖尿病、抗癌、抗骨质疏松、心脏保护、神经保护、肝脏保护、抗菌和抗寄生虫方面的潜在应用。氟化衍生物增强的生物活性，特别是抗菌、抗病毒和抗癌特性，归因于氟基团的引入，这增加了亲脂性和代谢稳定性。主要研究结果表明，氟化黄酮类化合物和查耳酮与抗生素具有协同作用，可抑制细菌外排泵，并显示出强大的抗病毒和抗癌特性。然而，细胞毒性和结构优化等挑战必须得到解决。文中讨论了氟化黄酮类化合物和查耳酮的合成，重点介绍了各种合成方法，如从氟化前体开始的缩合和环化反应，以及氟化策略，包括分子氟或氟化剂的使用。氟化黄酮类化合物和查耳酮是治疗药物开发的候选物，有克服耐药性的潜力。然而，需要进一步研究来调整它们的药理特性。
