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Marine-Derived Natural Lead Compound Disulfide-Linked Dimer Psammaplin A: Biological Activity and Structural Modification

机译:海洋衍生的天然铅化合物二硫键联的二聚体Psammaplin A:生物活性和结构修饰。

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摘要

Marine natural products are considered to be valuable resources that are furnished with diverse chemical structures and various bioactivities. To date, there are seven compounds derived from marine natural products which have been approved as therapeutic drugs by the U.S. Food and Drug Administration. Numerous bromotyrosine derivatives have been isolated as a type of marine natural products. Among them, psammaplin A, including the oxime groups and carbon–sulfur bonds, was the first identified symmetrical bromotyrosine-derived disulfide dimer. It has been found to have a broad bioactive spectrum, especially in terms of antimicrobial and antiproliferative activities. The highest potential indole-derived psammaplin A derivative, UVI5008, is used as an epigenetic modulator with multiple enzyme inhibitory activities. Inspired by these reasons, psammaplin A has gradually become a research focus for pharmacologists and chemists. To the best of our knowledge, there is no systematic review about the biological activity and structural modification of psammaplin A. In this review, the pharmacological effects, total synthesis, and synthesized derivatives of psammaplin A are summarized.
机译:海洋天然产物被认为是有价值的资源,具有多种化学结构和多种生物活性。迄今为止,有七种源自海洋天然产物的化合物已被美国食品和药物管理局批准用作治疗药物。已经分离出许多溴酪氨酸衍生物作为一种海洋天然产物。其中,psammaplin A(包括肟基和碳硫键)是首先鉴定出的对称溴代酪氨酸衍生的二硫键二聚体。已经发现它具有广泛的生物活性谱,特别是在抗微生物和抗增殖活性方面。潜在的最高吲哚衍生的psammaplin A衍生物UVI5008用作具有多种酶抑制活性的表观遗传调节剂。受这些原因的启发,psammaplin A已逐渐成为药理学家和化学家的研究重点。据我们所知,没有关于psammaplin A的生物学活性和结构修饰的系统评价。在这篇综述中,总结了psammaplin A的药理作用,总合成和合成衍生物。

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