State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032, China.
Chem Commun (Camb). 2010 Aug 14;46(30):5403-20. doi: 10.1039/c0cc00629g. Epub 2010 Jun 14.
The total synthesis of natural products "has to be viewed as an art and a science that needs to be advanced for its own sake" (K. C. Nicolaou) and indeed, the achievements within this field of chemistry during the last decades are astonishing. However, besides its inherent beauty, total synthesis also opens the gates widely to a better understanding of biological processes and the development of pharmaceutical interesting substances. Cyclic depsipeptides form one of the compound classes that have attracted tremendous attention from synthetic chemists. They often feature non-proteinogenic amino acids and various types of structural unique building blocks, which make them challenging targets for synthetic efforts. Their total synthesis offers the chance to implement the use of newly developed synthetic tools in a complex environment. Synthetic dead-ends have shown the limitations of today's chemistry as well as triggering the development of new methodologies to circumvent the observed problems. Cyclic depsipeptides also often possess biological properties, especially antimicrobial and antitumor activity, that make them promising candidates for further pharmaceutical investigations and thus have a value at their own. Furthermore, through construction from scratch, ambiguities regarding the structure of several members of that compound class could be successfully clarified and derivatives for structure-activity-relationship (SAR) studies obtained.
天然产物的全合成“必须被视为一门艺术和科学，需要为其自身的发展而推进”（K.C. Nicolaou），事实上，在过去几十年里，这一化学领域的成就令人惊叹。然而，除了其内在的美感之外，全合成也为更好地理解生物过程和开发具有药物应用价值的物质打开了大门。环肽是吸引合成化学家极大关注的化合物类别之一。它们通常含有非蛋白氨基酸和各种类型的结构独特的构建块，这使得它们成为合成努力的具有挑战性的目标。它们的全合成提供了在复杂环境中应用新开发的合成工具的机会。合成死胡同表明了当今化学的局限性，同时也引发了新方法学的发展，以规避观察到的问题。环肽还经常具有生物活性，特别是抗菌和抗肿瘤活性，这使它们成为进一步药物研究的有前途的候选物，因此具有自身的价值。此外，通过从头开始构建，可以成功澄清该化合物类别中几个成员的结构问题，并获得用于结构-活性关系（SAR）研究的衍生物。
