Macrocycles: MCR synthesis and applications in drug discovery

Eman M M Abdelraheem; Shabnam Shaabani; Alexander Dömling

doi:10.1016/j.ddtec.2018.06.008

Macrocycles: MCR synthesis and applications in drug discovery

Drug Discov Today Technol. 2018 Nov:29:11-17. doi: 10.1016/j.ddtec.2018.06.008. Epub 2018 Jul 12.

Authors

Eman M M Abdelraheem¹, Shabnam Shaabani², Alexander Dömling³

Affiliations

¹ University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands; Chemistry Department, Faculty of Science, Sohag University, Sohag, 82524, Egypt.
² University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands.
³ University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address: a.s.s.domling@rug.nl.

PMID: 30471668
DOI: 10.1016/j.ddtec.2018.06.008

Abstract

Macrocycles are an emerging and largely underexploited part of chemical space where potential drugs for difficult genomic targets can be discovered. Macrocycles can have advantages over their natural twins such as better control over synthesis, physicochemical properties and target binding. Fast and convergent synthesis pathways are underdeveloped. Multicomponent reaction (MCR) chemistry is very well suited for the synthesis of a diverse range of macrocycles and is also able to generate great levels of molecular diversity and complexity at low synthetic costs.

Publication types

Review

MeSH terms

Biological Products / chemistry
Chemistry, Pharmaceutical / methods*
Drug Discovery / methods*
Macrocyclic Compounds / chemical synthesis*
Molecular Targeted Therapy / methods
Pharmaceutical Preparations / chemical synthesis*

Substances

Biological Products
Macrocyclic Compounds
Pharmaceutical Preparations