Department of Pharmaceutical Engineering, School of Chemistry and Pharmaceutical Engineering, Huanghuai University, Zhumadian, Henan, People's Republic of China.
Arch Pharm (Weinheim). 2024 Oct;357(10):e2400344. doi: 10.1002/ardp.202400344. Epub 2024 Jun 29.
Breast cancer stands as the leading cause of cancer-related deaths among women globally, but current therapy is restricted to the serious adverse effects and multidrug resistance, necessitating the exploration of novel, safe, and efficient anti-breast cancer chemotherapeutic agents. Pyrazoles exhibit excellent potential for utilization as effective anti-breast cancer agents due to their ability to act on various biological targets. Particularly, pyrazole hybrids demonstrated the advantage of targeting multiple pathways, and some of them, which are exemplified by larotrectinib (pyrazolo[1,5-a]pyrimidine hybrid), can be applied for breast cancer therapy. Thus, pyrazole hybrids hold great promise as useful therapeutic interventions for breast cancer. The aim of this review is to summarize the current scenario of pyrazole hybrids with in vitro and/or in vivo anti-breast cancer potential, along with the modes of action and structure-activity relationships, covering articles published from 2020 to the present, to streamline the development of rational, effective and safe anti-breast cancer candidates.
乳腺癌是全球女性癌症相关死亡的主要原因，但目前的治疗方法受到严重不良反应和多药耐药性的限制，因此需要探索新型、安全、有效的抗乳腺癌化疗药物。由于能够作用于多种生物靶点，吡唑类化合物具有作为有效抗乳腺癌药物的巨大潜力。特别是，吡唑杂合体表现出靶向多种途径的优势，其中一些，如拉罗替尼（吡唑并[1,5-a]嘧啶杂合体），可用于乳腺癌治疗。因此，吡唑杂合体有望成为治疗乳腺癌的有用治疗干预措施。本综述的目的是总结具有体外和/或体内抗乳腺癌潜力的吡唑杂合体的现状，以及作用方式和构效关系，涵盖了 2020 年至今发表的文章，以简化合理、有效和安全的抗乳腺癌候选药物的开发。
