Phosphate linkers with traceable cyclic intermediates for self-immolation detection and monitoring.

Abstract

Self-immolation (SI) is the key principle of ProTide nucleotide prodrugs such as remdesivir, which is currently used to treat COVID-19 patients. Developing novel tailor-made SI systems requires new analytical methods for the detection and monitoring of SI. We developed a robust method for SI analysis using novel phosphate-based SI linkers with NMR traceable cyclic intermediates to distinguish SI from alternative fragmentation pathways and to monitor cargo release in real time.

• Authors: Eliška Procházková , Petr Šimon , Michal Straka , Juraj Filo , Michal Májek , Marek Cigáň , Ondřej Baszczyňski
• Journal: Chemical communications (Cambridge, England) (Chem Commun (Camb)) Vol. 57 Issue 2 Pg. 211-214 (Jan 07 2021) ISSN: 1364-548X [Electronic] England
• PMID: 33300900 (Publication Type: Journal Article)