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乳香酸:用于抗癌药物发现的先导化合物开发的优势结构。

Boswellic acids: privileged structures to develop lead compounds for anticancer drug discovery.

机构信息

Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Weinberg, Germany.

School of Pharmaceutical Sciences and Key Laboratory for Applied Technology of Sophisticated Analytical Instruments of Shandong Province, Shandong Analysis and Test Center, Qilu University of Technology (Shandong Academy of Sciences), Jinan, China.

出版信息

Expert Opin Drug Discov. 2021 Aug;16(8):851-867. doi: 10.1080/17460441.2021.1892640. Epub 2021 Mar 2.

Abstract

: Cancer has been identified to be the second major cause of death internationally as exemplified by ca. 9.6 million deaths in 2018 along with ca. 18 million new patients in 2018 that have been recorded. Natural boswellic acids (BAs) and their source, frankincense, have been reported to possess and anticancer effects toward various cancer cells.: This comprehensive review focuses on the importance of boswellic acids (BAs) for the establishment of future treatments of cancer. Moreover, potent semisynthetic derivatives of BAs have been described along with their mode of action. In addition, important structural features of the semisynthetic BAs required for cytotoxic effects are also discussed.: Numerous semisynthetic BAs illustrate excellent cytotoxic effects. Of note, compounds bearing cyanoenone moieties in ring A, endoperoxides and hybrids display increased and more potent cytotoxic effects compared with other semisynthetic BAs. Moreover, BAs have the potential to conjugate or couple with other anticancer compounds to synergistically increase their combined anticancer effects. In addition, to get derived BAs to become lead anticancer compounds, future research should focus on the preparation of ring A cyanoenones, endoperoxides, and C-24 amide analogs.

摘要

癌症已被确定为国际上的第二大死亡原因,例如,2018 年有大约 960 万人死亡,同年记录的新患者约为 1800 万。天然乳香酸(BAs)及其来源乳香已被报道具有针对各种癌细胞的 和 抗癌作用。

本综述重点介绍了乳香酸(BAs)在未来癌症治疗中的重要性。此外,还描述了 BAs 的有效半合成衍生物及其作用模式。此外,还讨论了半合成 BAs 发挥细胞毒性作用所需的重要结构特征。

许多半合成 BAs 表现出优异的细胞毒性作用。值得注意的是,在环 A 中带有氰基烯酮部分、内过氧化物和杂种的化合物与其他半合成 BAs 相比,显示出增加和更有效的细胞毒性作用。此外,BAs 有可能与其他抗癌化合物结合或偶联,以协同增强其联合抗癌作用。此外,为了使衍生的 BAs 成为潜在的抗癌化合物,未来的研究应集中在制备环 A 氰基烯酮、内过氧化物和 C-24 酰胺类似物上。

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