Neristatin 1是1991年从海洋动物总合草苔虫中分离得到的一个结构复杂而新颖、抗肿瘤活性显著 (IC50 = 1.58 nM) 的大环内酯类天然产物。由于neristatin 1含量甚微、来源困难，严重制约了其深入研究。目前，尚无其全合成、构效关系、以及深入的生物作用机制的报道。本项目以neristatin 1为研究对象，旨在发展一条高效易行的合成路线、完成其首次全合成，并构建其类似物库进行抗肿瘤活性研究、总结构效关系，为后续深入研究其生物作用机制，挖掘其潜在的治疗价值，为开发具有自主知识产权的创新药物奠定基础。

Neristatin 1, a novel and highly complex macrolide with potent antitumor activity (IC50 = 1.58 nM), was first isolated from marine animal Bugula neritina in 1991. The extremely low natural abundance of neristatin 1 has hampered its further studies. At present, no research on its total synthesis, structure-activity relationship for the antitumor activity, or further biological mechanism of action was reported. This project aims to develop an efficient and practical route for the total synthesis of neristatin 1 and construct its analogue library for SAR studies. This will pave the way for the studies on its antitumor mechanism of action and its potential therapeutic value, as well as developing innovative drugs with independent intellectual property rights.