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Macrocycles: Recent Advances in Synthesis, Reactivity, and Medicinal Chemistry

Maryam Barancheshme, Mozhan kakouei, Samad Khaksar





Introduction: A cyclic compound is common motif in natural product structures. Cyclic peptides, a vast subset of natural products, display a wide variety of biological activities. Owing to their size, cyclic peptides are particularly attractive scaffolds for interrogating challenging biomolecular interactions, such as those at protein–protein interfaces.


Methods and Results:

This review takes an overview of the literature for the synthesis of peptide and non-peptide macrocycles, concentrating on advances in the last five years up to the end of 2017. These methods are clustered by strategies for preparation and further derivatization of preformed macrocycle-containing building blocks. Examples of the use of macrocycles in medicinal chemistry are reported, including a collation of macrocycle derivatives appearing in recent patents for medicinal chemistry applications.


Scheme 1: Structure of the Complex of Human Programmed Death 1, PD-1, and Its Ligand PD-L1


This review aims to provide an overview of the extensive recent studies involving macrocycles in synthesis and medicinal chemistry and to highlight the continuing challenges.

Key words: Macrocycle; Peptide; Human Programmed Death 1; biomolecular

Grants: This research is supported by the Islamic Azad University, Ayatollah Amoli Branch.


DOI: https://doi.org/10.22037/ipa.v1i1.20056


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