氟具有独特的化学特性,如其强大的吸电子能力和小的原子尺寸,这使它成为药品设计和优化的宝贵资产。利用富含氟的药物来对抗癌症已经成为药物化学和药物发现中的一个突出方法,提供改善的临床结果和增强的药理特性。本综述探讨了2019年至今已批准的22种代表性含氟抗癌药物的合成方法和临床应用。揭示了他们的历史发展,品牌名称,药物靶标活性,作用机制,临床前药效学,临床疗效,和毒性。此外,该评论对所采用的代表性合成技术进行了广泛的分析。总的来说,这篇综述强调了将氟化学纳入抗癌药物研究的重要性,同时强调了在抗癌斗争中探索富含氟的化合物的前景。
Fluorine possesses distinctive chemical characteristics, such as its strong electron-withdrawing ability and small atomic size, which render it an invaluable asset in the design and optimization of pharmaceuticals. The utilization of
fluorine-enriched medications for combating cancer has emerged as a prominent approach in medicinal chemistry and drug discovery, offering improved clinical outcomes and enhanced pharmacological properties. This comprehensive review explores the synthetic approaches and clinical applications of approved 22 representative fluorinated anti-cancer drugs from 2019 to present, shedding light on their historical development, brand names, drug target activity, mechanism of action, preclinical pharmacodynamics, clinical efficacy, and toxicity. Additionally, the review provides an extensive analysis of the representative synthetic techniques employed. Overall, this review emphasizes the significance of incorporating
fluorine chemistry into anti-cancer drug research while highlighting promising future prospects for exploring compounds enriched with
fluorine in the battle against cancer.