Natural Product Inspired Scaffolds for Pharmaceutical Discovery

受天然产物启发的药物发现支架

• 批准号: 2099961
• 金额: --
• 依托单位: University of Southampton
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2018
• 资助国家: 英国
• 起止时间: 2018 至 无数据
• 项目状态: 已结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2099961
• 关键词: Natural; Product; Inspired; Scaffolds; Pharmaceutical

The project seeks to develop novel sustainable synthetic methods for assembly of bioactive compounds in a collaborative project with cancer sciences to identify inhibitors of metastatic cancer cells. Specifically, continuous photochemical and electrochemical synthetic methodology is to be developed and applied to the creation of heterocyclic core structures, which are present in a group of inhibitors. The project will investigate new synthetic strategies to heterocyclic core structures that are unsymmetrically substituted, and devise methods to react these in a selective fashion to produce candidates for evaluation as inhibitors of metastatic cancer cells. The "reagent free" approaches being investigated will deliver impact though new methodology to minimise chemical inputs into synthesis and manufacture, which is part of the EPSRC Dial-a-Molecule road-map. Existing synthetic approaches are highly restricted by the use of toxic and costly catalysts, or very low rates of production, which limit the quality and amount of material available and would ultimately render them unsuitable for manufacturing. The research will benefit from access to innovative electrochemical and photochemical flow reactors developed as part of the Programme Grant EP/P013341/1, which allow laboratory scale-up of key intermediates.

该项目旨在与癌症科学合作开发新型可持续合成方法，用于组装生物活性化合物，以识别转移性癌细胞的抑制剂。具体地说，连续的光化学和电化学合成方法将被开发并应用于产生杂环核心结构，这是存在于一组抑制剂。该项目将研究不对称取代的杂环核心结构的新合成策略，并设计以选择性方式反应这些结构的方法，以产生作为转移性癌细胞抑制剂的候选物。正在研究的“无试剂”方法将通过新方法产生影响，以最大限度地减少合成和制造中的化学输入，这是EPSRC Dial-a-Molecule路线图的一部分。现有的合成方法由于使用有毒和昂贵的催化剂或非常低的生产率而受到高度限制，这限制了可用材料的质量和数量，并最终使其不适合于制造。该研究将受益于作为EP/P013341/1计划资助的一部分开发的创新电化学和光化学流动反应器，这使得实验室扩大关键中间体。