SYNTHESIS OF MARINE DERIVED MACROCYCLIC SALICYLATES

海洋衍生大环水杨酸盐的合成

• 批准号: 7355164
• 负责人: JEF KAREL DE BRABANDER
• 金额: $ 0.06万
• 依托单位: WASHINGTON UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2006
• 资助国家: 美国
• 起止时间: 2006-02-01 至 2007-01-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7355164
• 关键词: SYNTHESIS; MARINE; DERIVED; MACROCYCLIC; SALICYLATES

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Natural products that elicit a specific biological response represent unique tools to identify, study, and target possible new gene products. Part of this research program is directed towards the design and synthesis of natural products that have unique actions on mammalian cells. In this context, we are developing a versatile total synthesis of salicylhalamides A-B and lobatamides A-F. These marine-derived macrocyclic salicylates represent a potentially new mechanistic class of antitumor compounds, and warrant the development of probe reagents for mechanism of action studies. In addition, only trace quantities of these secondary metabolites can be obtained from their natural source and neither these, nor any structurally related compounds, have been synthesized previously. An active interplay between chemical synthesis and cellular assays will pave the way for lead optimization efforts and an affinity-based search for the natural product's biological target.

该子项目是利用NIH/NCRR资助的中心赠款提供的资源的许多研究子项目之一。子弹和调查员（PI）可能已经从其他NIH来源获得了主要资金，因此可以在其他清晰的条目中代表。列出的机构适用于该中心，这不一定是调查员的机构。引起特定生物响应的天然产品代表了识别，研究和靶向可能的新基因产品的独特工具。该研究计划的一部分是针对对哺乳动物细胞具有独特作用的天然产品的设计和合成。在这种情况下，我们正在开发水杨酰胺A-B和Lobatamides A-F的多功能总合成。这些海洋衍生的大环水杨酸盐代表了一种潜在的抗肿瘤化合物机械类别，并保证开发探针试剂以进行作用机理。此外，仅此这些二级代谢产物可以从其自然来源获得，并且这些二次代谢物既不是先前合成的，否则这些化合物或任何与结构相关的化合物均未得到合成。化学合成和细胞测定之间的主动相互作用将为铅优化工作和基于亲和力的搜索自然产物的生物靶标铺平道路。