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过去十年中关于 lamellarin 的合成和构效关系的研究进展。

Progress on synthesis and structure-activity relationships of lamellarins over the past decade.

机构信息

School of Pharmaceutical Science, Zhejiang Chinese Medical University, 310061, Hangzhou, China.

Cité scolaire Fesch, 5 cours Grandval, 20000 Ajaccio, France.

出版信息

Eur J Med Chem. 2024 Apr 5;269:116294. doi: 10.1016/j.ejmech.2024.116294. Epub 2024 Mar 6.

Abstract

Lamellarins are polyaromatic alkaloids isolated from marine organisms, including mollusks, tunicates, and sponges. Currently, over 60 structurally distinct natural lamellarins have been reported, and most of them exhibit promising biological activities, such as topoisomerase inhibition, mitochondrial function inhibition, multidrug resistance reversing, and anti-HIV activity. There has also been a significant progress on the synthetic study of lamellarins which has been regularly updated by numerous medicinal chemists as well. This review provides a detailed summary of the synthesis, pharmacology, and structural modification of lamellarins over the past decades.

摘要

层叠海兔素是从海洋生物(包括软体动物、被囊动物和海绵)中分离出来的多环生物碱。目前,已经报道了 60 多种结构不同的天然层叠海兔素,其中大多数具有有前景的生物活性,如拓扑异构酶抑制、线粒体功能抑制、多药耐药逆转和抗 HIV 活性。层叠海兔素的合成研究也取得了显著进展,许多药物化学家定期对此进行更新。本文综述了过去几十年中层叠海兔素的合成、药理学和结构修饰方面的研究进展。

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