Synthesis of Betulinic Acid Derivatives with Modified A‐Rings and their Application as Potential Drug Candidates,Asian Journal of Organic Chemistry

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Synthesis of Betulinic Acid Derivatives with Modified A‐Rings and their Application as Potential Drug Candidates
Asian Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2018-06-19 , DOI: 10.1002/ajoc.201800163
Lucie Borkova ₁ , Jiri Hodon ₁ , Milan Urban ₁

Affiliation

This Focus Review summarizes recent advances in the synthesis of betulinic acid derivatives with modified A‐rings. It also focuses on their application as potential therapeutic agents for the treatment of cancer and other diseases. Betulinic acid (BA) exhibits therapeutically interesting biological properties, including antitumor, anti‐HIV, antiprotozoal, and hepato‐ or nephroprotective activity; however, its clinical use has been severely limited by its higher IC₅₀ value and worse pharmacological parameters than the currently used drugs. On the other hand, semisynthetic analogues of BA are much better suited for potential clinical use. Among these analogues, compounds that contain a modified A‐ring are the most promising. We hope that this Focus Review will serve as a guide for the synthesis of new BA derivatives with applications as drug candidates. A general audience may also find this Focus Review interesting, because it describes the structural motifs that are responsible for the observed bioactivities.

中文翻译：

具有修饰的A环的桦木酸衍生物的合成及其作为潜在候选药物的应用

本《聚焦评论》总结了合成具有修饰的A环的桦木酸衍生物的最新进展。它还侧重于将它们用作治疗癌症和其他疾病的潜在治疗剂的应用。桦木酸（BA）表现出具有治疗意义的生物学特性，包括抗肿瘤，抗HIV，抗原生动物和肝或肾保护活性。然而，其较高的IC ₅₀严重限制了其临床应用的价值和比目前使用的药物更差的药理学参数。另一方面，BA的半合成类似物更适合潜在的临床应用。在这些类似物中，含有修饰的A环的化合物是最有前途的。我们希望本《聚焦评论》将作为合成新的BA衍生物和候选药物的指南。普通读者也可能会发现本《聚焦评论》很有趣，因为它描述了负责观察到的生物活性的结构基序。

更新日期：2018-06-19

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