Anticancer activities, structure–activity relationship, and mechanism of action of 12-, 14-, and 16-membered macrolactones,Archiv der Pharmazie

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Anticancer activities, structure–activity relationship, and mechanism of action of 12-, 14-, and 16-membered macrolactones
Archiv der Pharmazie ( IF 4.3 ) Pub Date : 2021-06-17 , DOI: 10.1002/ardp.202100025
Ruo Wang ₁

Affiliation

Cancer remains one of the major causes of death worldwide despite the encouraging breakthroughs in the discovery of novel chemotherapeutic agents in recent years. The development of new effective anticancer candidates still represents a challenging endeavor due to the severe anticancer demands and the emergence of drug-resistant, especially multidrug-resistant, cancers. Macrolactones could regulate multiple signaling pathways in cancer cells and demonstrated potential anticancer effects, including inhibition of proliferation, metastasis, and angiogenic activity. Accordingly, macrolactones possess excellent efficacy against both drug-sensitive and drug-resistant cancer cells, and the rational design of macrolactones may provide valuable therapeutic interventions for cancers. The purpose of this review is as follows: (1) outline the recent advances made in the development of 12-, 14-, and 16-membered macrolactones with anticancer potential; (2) summarize the structure–activity relationship; and (3) discuss their anticancer mechanisms.

中文翻译：

12-、14-和16-元大环内酯的抗癌活性、构效关系和作用机制

尽管近年来在发现新型化学治疗剂方面取得了令人鼓舞的突破，但癌症仍然是全球死亡的主要原因之一。由于严重的抗癌需求和耐药性，尤其是多重耐药性癌症的出现，开发新的有效抗癌候选物仍然是一项具有挑战性的工作。大环内酯可以调节癌细胞中的多种信号通路，并显示出潜在的抗癌作用，包括抑制增殖、转移和血管生成活性。因此，大环内酯对药物敏感和耐药癌细胞均具有优异的疗效，大环内酯的合理设计可为癌症提供有价值的治疗干预。本次审查的目的如下：(1) 概述在开发具有抗癌潜力的 12 元、14 元和 16 元大环内酯方面取得的最新进展；(2) 总结构效关系；(3) 讨论它们的抗癌机制。

更新日期：2021-06-17

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