Shanghai Jiao Tong University School of Medicine, Shanghai, China.
Shengli Clinical College of Fujian Medical University, Department of Pharmacy, Fujian Provincial Hospital, Fuzhou, China, Fuzhou, China.
Arch Pharm (Weinheim). 2024 Oct;357(10):e2400438. doi: 10.1002/ardp.202400438. Epub 2024 Jul 9.
Globally, breast cancer (BC) has the highest prevalence among malignant diseases. BC is also the primary cause of death among women. Notably, BC morbidity has been increasing continuously at an approximate growth rate of 2.2% per year. Persistent BC is a major public health issue worldwide. Consequently, novel chemotherapeutic agents to combat this lethal disease should be developed urgently. Coumarins with interesting structural and mechanistic variations exhibit promising activity in several forms of BC, including BCs with multidrug resistance. In particular, coumarin hybrids composed of coumarin and one or more anti-BC pharmacophores can target different biological components in BC cells simultaneously. Thus, coumarin hybrids are useful scaffolds that can help improve the anti-BC efficacy of coumarins, reduce side effects, improve pharmacokinetics, minimize drug-drug interactions, and circumvent drug resistance. This review, in which articles published from 2020 to the present day have been evaluated, highlights the landscape of coumarin hybrids that exhibit therapeutic effects against breast cancer. These findings can aid further investigations on novel antibreast-cancer therapeutics.
在全球范围内,乳腺癌(BC)是最常见的恶性疾病。BC 也是女性死亡的主要原因。值得注意的是,BC 的发病率一直在以每年约 2.2%的速度持续增长。持续性 BC 是全球主要的公共卫生问题。因此,迫切需要开发新的化疗药物来对抗这种致命疾病。具有有趣结构和机制变化的香豆素在几种形式的 BC 中表现出有希望的活性,包括具有多药耐药性的 BC。特别是,由香豆素和一个或多个抗 BC 药效团组成的香豆素杂合体能同时针对 BC 细胞中的不同生物成分。因此,香豆素杂合体是有用的支架,可以帮助提高香豆素的抗 BC 功效,减少副作用,改善药代动力学,最小化药物相互作用,并规避耐药性。本综述评估了 2020 年至今发表的文章,重点介绍了具有治疗乳腺癌疗效的香豆素杂合体的研究现状。这些发现可以帮助进一步研究新型抗乳腺癌治疗药物。