布洛芬是临床上最常用的非甾体类抗炎药之一，具有抗炎、镇痛等多种药理活性。近年来，布洛芬抗肿瘤活性受到广泛的关注。但由于布洛芬缺乏选择性、水溶性差且结构中具有游离的羧基会引起胃肠道的不良反应从而限制了其在抗癌治疗中的进一步应用，此外布洛芬抗癌的作用机制尚未完全阐明。因此，为了提高布洛芬生物利用度，改善不良反应并寻找新靶点，研究人员通过各种方法设计合成新的布洛芬衍生物。对具有抗肿瘤活性的布洛芬酰胺衍生物、酯类衍生物、金属复合物及其他衍生物的研究进展进行综述，为后续布洛芬结构修饰物作为抗肿瘤药物的研究、开发和利用提供借鉴和参考。

Ibuprofen, one of the most commonly used nonsteroidal anti-inflammatory drugs in clinic, has anti-inflammatory, analgesic and other pharmacological activities. In recent years, its anti-tumor activity has received extensive attention. However, due to the lack of selectivity and water solubility of ibuprofen, as well as the presence of free carboxyl groups in its structure that can cause adverse reactions in the gastrointestinal tract, its further application in anti-tumor therapy is limited. In addition, the anti-tumor mechanism of ibuprofen is not completely elucidated. Therefore, in order to improve the bioavailability and adverse effects of ibuprofen and to find new targets, researchers have designed and synthesized new ibuprofen derivatives by various methods. In this paper, the research progress of ibuprofen amide derivatives, ester derivatives, metal complexes and other derivatives with antitumor activity is reviewed to provide reference for the subsequent research, development and utilization of ibuprofen structural modifiers as anti-tumor drugs.

R979.1

湖南省自然科学基金项目（2022JJ80089）;2023年度湖南省大学生创新创业训练计划一般项目（湘教通〔2023〕237号-S202310541073）