金诺芬 (AF) 是一种成熟的、经 FDA 批准的抗关节炎黄金药物，目前正在通过药物重新利用来重新评估其多种治疗适应症。 AF 作为一种潜在的抗癌药物显示出巨大的前景，并已被批准用于一些癌症临床试验。人们对 AF 重新产生的兴趣引发了对金诺芬类似物的设计、制备和生物学评价的广泛研究，金诺芬类似物可能具有比母体药物更好的药理学特征。本文综述了 AF 支架的化学修饰策略。过去 20 年来，已经制备并表征了几种金诺芬类似物，用于癌症治疗领域的医学应用。提出并讨论了一些新兴的结构-功能关系。近年来，AF 支架的化学修饰一直是热门话题，这种策略导致了几种 AF 类似物的制备和评估。碘道诺芬的案例是一个特别有希望的例子。一组 AF 衍生物的同质生物学数据的可用性允许提出一些初步的结构-功能关系，这可能会激发设计和合成用于癌症治疗的新的、更好的 AF 类似物。

Auranofin (AF) is a well-established, FDA-approved, antiarthritic gold drug that is currently being reevaluated for a variety of therapeutic indications through drug repurposing. AF has shown great promise as a potential anticancer agent and has been approved for a few clinical trials in cancer. The renewed interest in AF has led to extensive research into the design, preparation and biological evaluation of auranofin analogs, which may have an even better pharmacological profile than the parent drug.This article reviews the strategies for chemical modification of the AF scaffold. Several auranofin analogs have been prepared and characterized for medical application in the field of cancer treatment over the last 20 years. Some emerging structure-function relationships are proposed and discussed.The chemical modification of the AF scaffold has been the subject of intense activity in recent years and this strategy has led to the preparation and evaluation of several AF analogs. The case of iodauranofin is a particularly promising example. The availability of homogeneous biological data for a group of AF derivatives allows some initial structure-function relationships to be proposed, which may inspire the design and synthesis of new and better AF analogs for cancer treatment.