Published November 23, 2020
| Version v1
Journal article
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Phosphate linkers with traceable cyclic intermediates for self-immolation detection and monitoring
Authors/Creators
- 1. Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences
- 2. Faculty of Science, Charles University
- 3. Department of Organic Chemistry, Faculty of Natural Sciences, Comenius University
Description
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.