多肽类化合物具有丰富的结构多样性和生物活性，是重要的药物来源。近年来，多肽类化合物在调控细胞内的蛋白-蛋白相互作用的领域显示出巨大的药用潜力，进一步在化学和制药领域取得了广泛的关注。环状结构的引入往往可以提高多肽类化合物的细胞穿透性，增强其体内环境中的稳定性，增强其对于靶标的亲和识别能力。尽管取得了一定成功，现有的化学修饰/环化策略仍存在着若干局限性，如对非天然氨基酸和含有高反应活性基团的氨基酸的依赖等。本项目旨在发展有效的化学方法，通过对氨基酸侧链中“化学惰性”的C-H键进行活化，使其参与到环肽结构的构建中，制备一系列具有新颖结构的环肽化合物，进一步拓展现有环肽化合物的结构多样性，并筛选出具有新颖生物活性的环肽分子。

Peptides and peptidomimics are attracting increasing attention in both the chemical and pharmaceutical community as a rich source of drug candidates and/or biological tools, especially due to their potency to interrupt biological events mediated by protein-protein interactions. Despite the success achieved in this field, limitations remain to be overcome, including the requirement for the incorporation of unnatural amino acids and reactive amino acid side chains. This project will focus on the development of efficient methodology to synthesize cyclic peptides by macrocyclization using C-H activation. With this methodology, we will prepare cyclic peptides with novel architectures and biological importance.