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The synthesis and biological activity of marine alkaloid derivatives and analogues

机译：海洋生物碱衍生物和类似物的合成与生物活性

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The ocean is the origin of life, with a unique ecological environment, which has given birth to a wealth of marine organisms. The ocean is an important source of biological resources and tens of thousands of monomeric compounds have been separated from marine organisms using modern separation technology. Most of these monomeric compounds have some kind of biological activity that has attracted extensive attention from researchers. Marine alkaloids are a kind of compound that can be separated from marine organisms. They have complex and special chemical structures, but at the same time, they can show diversity in biological activities. The biological activities of marine alkaloids mainly manifest in the form of anti-tumor, anti-fungus, anti-viral, anti-malaria, and anti-osteoporosis properties. Many marine alkaloids have good medicinal prospects and can possibly be used as anti-tumor, anti-viral, and anti-fungal clinical drugs or as lead compounds. The limited amounts of marine alkaloids that can be obtained by separation, coupled with the high cytotoxicity and low selectivity of these lead compounds, has restricted the clinical research and industrial development of marine alkaloids. Marine alkaloid derivatives and analogues have been obtained via rational drug design and chemical synthesis, to make up for the shortcomings of marine alkaloids; this has become an urgent subject for research and development. This work systematically reviews the recent developments relating to marine alkaloid derivatives and analogues in the field of medical chemistry over the last 10 years (2010–2019). We divide marine alkaloid derivatives and analogues into five types from the point-of-view of biological activity and elaborated on these activities. We also briefly discuss the optimization process, chemical synthesis, biological activity evaluation, and structure–activity relationship (SAR) of each of these compounds. The abundant SAR data provides reasonable approaches for the design and development of new biologically active marine alkaloid derivatives and analogues.
机译：海洋是生命的起源，具有独特的生态环境，它赋予了丰富的海洋生物。海洋是生物资源的重要来源，使用现代分离技术分离了数万种单体化合物。大多数这些单体化合物具有某种生物活性，这些生物活性引起了研究人员的广泛关注。海洋生物碱是一种可以与海洋生物分离的化合物。它们具有复杂和特殊的化学结构，但同时，它们可以在生物活动中表现出多样性。海洋生物碱的生物活性主要以抗肿瘤，抗真菌，抗病毒，抗疟疾和抗骨质疏松性能的形式显现。许多海洋生物碱具有良好的药用前景，并且可能用作抗肿瘤，抗病毒和抗真菌临床药物或作为铅化合物。可以通过分离获得的有限量的海洋生物碱，与这些铅化合物的高细胞毒性和低选择性相结合，限制了海洋生物碱的临床研究和工业发展。通过合理的药物设计和化学合成获得了海洋生物碱衍生物和类似物，以弥补海洋生物碱的缺点;这已成为研发的紧急主题。这项工作系统地审查了过去10年（2010-2019）的医学化学领域中有关海洋生物碱衍生物和类似物的最新发展。从生物活性的观点来看，我们将海洋生物碱衍生物和类似物分为五种类型，并阐述这些活动。我们还简要介绍了这些化合物中每种化合物的优化过程，化学合成，生物活性评价和结构 - 活性关系（SAR）。丰富的SAR数据为新的生物活性海洋生物碱衍生物和类似物的设计和开发提供了合理的方法。

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