Ageladine A,一种溴吡咯生物碱,取自海绵中村Agelas

Compounds Pub Date : 2023-01-19 DOI:10.3390/compounds3010010
George E. Magoulas
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引用次数: 0

摘要

在过去的三十年中,海洋次生代谢物已成为生物活性化合物的重要来源。在探索的海洋生物中,海绵提供了大量的代谢物,具有独特的结构多样性和过多的生物活性。Ageladine A是一种从海绵Agelas nakamurai中分离得到的溴吡咯类荧光生物碱,具有抑制基质金属蛋白酶(MMP)和抗血管生成的活性。由于这种有趣的生物学特征,Ageladine A在发现后不久就成为全合成的靶标。此外,还合成了大量的衍生物,并对其生物活性进行了评价。本综述重点介绍了合成阿格拉定a的所有成功的努力。此外,还介绍了所有用于鉴定和评估新的更有效的抑制剂以及阐明其活性的结构特征的药物化学方法。
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Ageladine A, a Bromopyrrole Alkaloid from the Marine Sponge Agelas nakamurai
During the last three decades, secondary metabolites of marine origin have emerged as a significant source of bioactive compounds. Among the marine organisms explored, sponges offer a vast number of metabolites with unique structural diversity and a plethora of biological activities. Ageladine A, a fluorescent bromopyrrole alkaloid isolated from the marine sponge Agelas nakamurai, exhibited matrix metalloproteinase (MMP) inhibitory properties, as well as antiangiogenic activity. Due to this interesting biological profile, Ageladine A became, soon after its discovery, a target for total synthesis. In addition, a significant number of derivatives have been synthesized, and their biological activity was evaluated. The present review highlights all the successful efforts made towards the synthesis of Ageladine A. Furthermore, all the medicinal chemistry approaches to identify and assess new more potent inhibitors and to elucidate the structural features responsible for the activity are described.
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