关键词: breast cancer coumarin hybrid molecules mechanisms of action structure–activity relationship

来  源:   DOI:10.1002/ardp.202400438

Abstract:
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.
摘要:
全球范围内,乳腺癌(BC)在恶性疾病中患病率最高。BC也是女性死亡的主要原因。值得注意的是,BC发病率一直以每年约2.2%的增长率持续增加。持续BC是世界范围内的主要公共卫生问题。因此,应该紧急开发新的化疗药物来对抗这种致命的疾病。香豆素具有有趣的结构和机理变化,在几种形式的BC中表现出有希望的活性,包括具有多重耐药性的BCs。特别是,由香豆素和一种或多种抗BC药效团组成的香豆素杂种可以同时靶向BC细胞中的不同生物组分。因此,香豆素杂种是有用的支架,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,尽量减少药物-药物相互作用,规避耐药性。这次审查,其中对2020年至今发表的文章进行了评估,突出显示对乳腺癌具有治疗作用的香豆素杂种的景观。这些发现可以帮助对新型抗乳腺癌疗法的进一步研究。
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