Synthetic Tools that Enable Synthesis and Understanding of Bioactive Macrocycles

Abstract

This article aims to summarizing the evolution of my lab’s research efforts in making and understanding peptide macrocycles. What started as a curiosity-driven investigation of amphoteric structures in multicomponent reactions, has turned into a sustained exploration of complex macrocyclic peptides. As part of this journey, my students and I have introduced new tools that enable chemical synthesis and property-driven optimization of cyclic peptides. These contributions are expected to be relevant in the areas of drug discovery and biological probe design.