Total synthesis of biologically active lactone/lactam natural products

生物活性内酯/内酰胺天然产物的全合成

• 批准号: EP/Y026888/1
• 负责人: Jonathan Burton
• 金额: $ 25.55万
• 依托单位: University of Oxford
• 依托单位国家: 英国
• 项目类别: Fellowship
• 财政年份: 2023
• 资助国家: 英国
• 起止时间: 2023 至 无数据
• 项目状态: 未结题
• 来源: https://gtr.ukri.org/projects?ref=EP%2FY026888%2F1
• 关键词: Total; synthesis; biologically; active; lactone

Natural products provide a rich source of biologically active molecules for the improvement of human health. In the area of cancer, 65% of all anticancer drugs are natural products or derivatives thereof, while the increasingly important area of anti-infectives has been dependent on natural products and derivatives. This proposal concerns the total synthesis and full biological evaluation of a family of structurally and stereochemically complex natural products with a range of biological activities including antibiotic and anticancer activity. The complex natural products can be readily broken down into four key fragments some of which have been previously synthesis using key oxidative cyclisation methodology and tin-free cross coupling methods. Developing methods for the assembly of these four key fragments into the final target molecules is one of the key objectives of the project which should then allow numerous members of the family to be synthesised and their full biological profile assessed.

天然产物为改善人类健康提供了丰富的生物活性分子来源。在癌症领域，65%的抗癌药物是天然产物或其衍生物，而日益重要的抗感染领域也依赖于天然产物及其衍生物。该提案涉及一系列结构和立体化学复杂的天然产物的全合成和全面生物学评价，这些天然产物具有一系列生物活性，包括抗生素和抗癌活性。复杂的天然产物可以很容易地分解成四个关键片段，其中一些片段之前已经使用关键的氧化环化方法和无锡交叉偶联方法合成。开发将这四个关键片段组装成最终目标分子的方法是该项目的关键目标之一，该项目随后将允许合成该家族的众多成员并评估其完整的生物学特征。